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(Floxin; Ocuflox)
Ofloxacin is a fluoroquinolone whose primary mechanism of action is inhibition of bacterial DNA gyrase.
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Ofloxacin
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Tedizolid is the active moiety of the prodrug tedizolid phosphate, with high potency against Gram-positive species.
IC50 Value: N/A
Target: Antibacterial
The MIC(50) and MIC(90) of tedizolid against both methicillin-susceptible S. aureus (MSSA) and MRSA were 0.25 μg/ml, compared with a MIC(50) of 1 μg/ml and MIC(90) of 2 μg/ml for linezolid. For coagulase-negative staphylococci (n = 7), viridans group streptococci (n = 15), and beta-hemolytic streptococci (n = 3), the MICs ranged from 0.03 to 0.25 μg/ml for tedizolid and from 0.12 to 1 μg/ml for linezolid.
Torezolid (also known as TR-701 and now tedizolid) is an oxazolidinone drug in phase-II clinical trials for complicated skin and skin-structure infections (cSSSI), including those caused by Methicillin-resistant Staphylococcus aureus (MRSA). From Wikipedia
5-hydroxypyrazine-2-carboxylic acid , a metabolite of anti-tuberculosis drug pyrazinamide (PZA).
Dactinomycin D(Actinomycin D; Oncostatin K) is the most significant member of actinomycines, which are a class of polypeptide antibiotics isolated from soil bacteria of the genus Streptomyces.
IC50 value:
Target: RNA polymerase; DNA/RNA synthesis
Actinomycin D was the first antibiotic shown to have anti-cancer activity. Actinomycin D is shown to have the ability to inhibit transcription. Actinomycin D does this by binding DNA at the transcription initiation complex and preventing elongation of RNA chain by RNA polymerase.
AHAS inhibitor is a novel acetohydroxyacid synthase(AHAS) inhibitor, a promising drug target against Mycobacterium tuberculosis (MTB).
IC50 value:
Target: acetohydroxyacid synthase; antibacterial
Amikacin(BAY416651) is a semi-synthetic aminoglycoside antibiotic derived from kanamycin A.
Target: Antibacterial
Amikacin disrupts bacterial protein synthesis by binding to the 30S ribosome of susceptible organisms. Binding interferes with mRNA binding and tRNA acceptor sites leading to the production of non-functional or toxic peptides. Other mechanisms not fully understood may confer the bactericidal effects of amikacin. Amikacin is also nephrotoxic and ototoxic. Amikacin is useful against gentamicin-resistant gram-negative bacilli and also in the treatment of infections caused by susceptible Nocardia and nontuberculous mycobacteria.[1].
Amikacin Hydrate(BAY416651 hydrate) is a semi-synthetic aminoglycoside antibiotic derived from kanamycin A.
Target: Antibacterial
Amikacin Hydrate is a semi-synthetic aminoglycoside antibiotic derived from kanamycin A. Amikacin disrupts bacterial protein synthesis by binding to the 30S ribosome of susceptible organisms. Binding interferes with mRNA binding and tRNA acceptor sites leading to the production of non-functional or toxic peptides. Other mechanisms not fully understood may confer the bactericidal effects of amikacin. Amikacin is also nephrotoxic and ototoxic. Amikacin is useful against gentamicin-resistant gram-negative bacilli and also in the treatment of infections caused by susceptible Nocardia and nontuberculous mycobacteria.[1].
Amikacin sulfate(BAY416651 sulfate) is a semi-synthetic aminoglycoside antibiotic derived from kanamycin A.
Target: Antibacterial
Amikacin disrupts bacterial protein synthesis by binding to the 30S ribosome of susceptible organisms. Binding interferes with mRNA binding and tRNA acceptor sites leading to the production of non-functional or toxic peptides. Other mechanisms not fully understood may confer the bactericidal effects of amikacin. Amikacin is also nephrotoxic and ototoxic. Amikacin is useful against gentamicin-resistant gram-negative bacilli and also in the treatment of infections caused by susceptible Nocardia and nontuberculous mycobacteria.[1].
Amoxicillin is a moderate- spectrum, bacteriolytic, β-lactam antibiotic.
Target: Antibacterial
Amoxicillin is a moderate-spectrum, bacteriolytic, β-lactam antibiotic in the aminopenicillin family used to treat bacterial infections caused by susceptible Gram-positive and Gram-negative microorganisms. It is usually the drug of choice within the class because it is better-absorbed, following oral administration, than other β-lactam antibiotics. Amoxicillin is susceptible to degradation by β-lactamase-producing bacteria, which are resistant to a narrow spectrum of β-lactam antibiotics, such as penicillin. For this reason, it is often combined with clavulanic acid, a β-lactamase inhibitor. This increases effectiveness by reducing its susceptibility to β-lactamase resistance. From Wikipedia.
Amoxicillin Sodium is a moderate- spectrum, bacteriolytic, β-lactam antibiotic.
Target: Antibacterial
Amoxicillin is a moderate-spectrum, bacteriolytic, β-lactam antibiotic in the aminopenicillin family used to treat bacterial infections caused by susceptible Gram-positive and Gram-negative microorganisms. It is usually the drug of choice within the class because it is better-absorbed, following oral administration, than other β-lactam antibiotics. Amoxicillin is susceptible to degradation by β-lactamase-producing bacteria, which are resistant to a narrow spectrum of β-lactam antibiotics, such as penicillin. For this reason, it is often combined with clavulanic acid, a β-lactamase inhibitor. This increases effectiveness by reducing its susceptibility to β-lactamase resistance. From Wikipedia.
Amoxicillin Trihydrate is a moderate- spectrum, bacteriolytic, β-lactam antibiotic.
Target: Antibacterial
Amoxicillin is a moderate-spectrum, bacteriolytic, β-lactam antibiotic in the aminopenicillin family used to treat bacterial infections caused by susceptible Gram-positive and Gram-negative microorganisms. It is usually the drug of choice within the class because it is better-absorbed, following oral administration, than other β-lactam antibiotics. Amoxicillin is susceptible to degradation by β-lactamase-producing bacteria, which are resistant to a narrow spectrum of β-lactam antibiotics, such as penicillin. For this reason, it is often combined with clavulanic acid, a β-lactamase inhibitor. This increases effectiveness by reducing its susceptibility to β-lactamase resistance. From Wikipedia.
Ampicillin is an orally active broad-spectrum antibiotic.
Target: Antibacterial
Ampicillin is an antibiotic useful for the treatment of a number of bacterial infections. It is a beta-lactam antibiotic that is part of the aminopenicillin family and is roughly equivalent to its successor, amoxicillin in terms of spectrum and level of activity. Belonging to the penicillin group of beta-lactam antibiotics, ampicillin is able to penetrate Gram-positive and some Gram-negative bacteria. It differs from penicillin G, or benzylpenicillin, only by the presence of an amino group. That amino group helps the drug penetrate the outer membrane of Gram-negative bacteria. Ampicillin acts as an irreversible inhibitor of the enzyme transpeptidase, which is needed by bacteria to make their cell walls. It inhibits the third and final stage of bacterial cell wall synthesis in binary fission, which ultimately leads to cell lysis. Ampicillin has received FDA approval for its mechanism of action. From Wikipedia.
Ampicillin Sodium is an orally active broad-spectrum antibiotic.
Target: Antibacterial
Ampicillin is an antibiotic useful for the treatment of a number of bacterial infections. It is a beta-lactam antibiotic that is part of the aminopenicillin family and is roughly equivalent to its successor, amoxicillin in terms of spectrum and level of activity. Belonging to the penicillin group of beta-lactam antibiotics, ampicillin is able to penetrate Gram-positive and some Gram-negative bacteria. It differs from penicillin G, or benzylpenicillin, only by the presence of an amino group. That amino group helps the drug penetrate the outer membrane of Gram-negative bacteria. Ampicillin acts as an irreversible inhibitor of the enzyme transpeptidase, which is needed by bacteria to make their cell walls. It inhibits the third and final stage of bacterial cell wall synthesis in binary fission, which ultimately leads to cell lysis. Ampicillin has received FDA approval for its mechanism of action. From Wikipedia.
Apramycin(Nebramycin II) is an aminoglycoside antibiotic used in veterinary medicine.
IC50 value:
Target: Apramycin stands out among aminoglycosides for its mechanism of action which is based on blocking translocation and its ability to bind also to the eukaryotic decoding site despite differences in key residues required for apramycin recognition by the bacterial target. The drug binds in the deep groove of the RNA which forms a continuously stacked helix comprising non-canonical C.A and G.A base pairs and a bulged-out adenine. The binding mode of apramycin at the human decoding-site RNA is distinct from aminoglycoside recognition of the bacterial target, suggesting a molecular basis for the actions of apramycin in eukaryotes and bacteria.
Avibactam is a non-β-lactam β-lactamase inhibitor antibiotic.
IC50 value:
Target: antibacterial; β-lactamase inhibitor
Avibactam is a novel investigational non-beta-lactam beta-lactamase inhibitor that is being developed for possible use in combination with ceftaroline in the U.S. Avibactam does not have any intrinsic antibacterial activity in its own right, but appears to be capable of inhibiting beta-lactamase enzymes that belong to molecular classes A and C.Avibactam is useful for Antibiotics.
AVX 13616 shows the potent in vivo antibacterial activity of Avexa’s lead antibacterial candidate; particularly against drug-resistant Staphylococcus pathogens.
IC50 value: 2-4 ug/ml (MICs)
Target: antibacterial agent
AVX13616 was as active as mupirocin in a nasal decolonization model but required only a single application. The compounds are being developed for topical indications and/or wound infection/catheter-related infections. AVX13616 and other compounds showed broad spectrum antibacterial activity against a range of isolates with MICs of 2-4 micrograms per millilitre against S. aureus, coagulase negative staphylococci, enterococci, MRSA, VISA and VRSA. A single application of 5% (w/w) AVX13616 (approximately equimolar to 2% mupirocin) was as effective as 2% mupirocin administered twice a day for five days in nasal decolonisation of MRSA in mice.
Azithromycin, derived from erythromycin, is a antibiotic. Azithromycin binds to the 50S subunit of the bacterial ribosome, and thus inhibits translation of mRNA.
IC50 Value:
Target: Antibacterial
Azithromycin is an azalide, a subclass of macrolide antibiotics. Azithromycin is one of the world's best-selling antibiotics.
in vitro: The geometric mean 50% inhibitory concentration (IC50) of azithromycin was 2,570.3 (95% CI=2,175.58 to 3,036.58) ng/ml [1]. Azithromycin, clarithromycin and roxithromycin inhibited the proliferation of both the concanavalin A- and superantigen-stimulated PBMCs dose-dependently. The effect of azithromycin was the strongest, with IC50 values of less than 5 ?g/ml [2].
in vivo: Azithromycin produced a slightly higher percentage of patients with a greater than 80% reduction in their inflammatory acne lesions (85.7%) vs. an average of 77.1% for all other agents [3].
Clinical trial:
Azlocillin is an acylampicillin with a broad spectrum against bacteria.
Target: Antibacterial
Azlocillin (12.5 μg/mL) inhibits over 75% of the isolates of Pseudomonas aeruginosa. Azlocillin (12.5 μg/mL) is also active against indole-negative and -positive Proteus spp., inhibiting 98 and 71%, respectively. Azlocillin is more active than mezlocillin, ticarcillin, and carbenicillin and as active as BLP-1654 against isolates of P. aeruginosa [1]. The acyl side chains of Azlocillin have an ureido-(urea) structurehence the name "ureidopenicillins" or, more specifically, "acylureidopenicillins." In vitro studies against P. aeruginosa demonstrates that piperacillin has activity that is twice that of azlocillin, 4 times that of mezlocillin and ticarcillin, and about 8 times that of carbenicillin. Azlocillin produces elongated bacterial forms with delayed or no lysis in morphologic studies [2].
Azlocillin has MICs of 12.5 μg/mL on Pseudomonas aeruginosa. Azlocillin (3.125 μg/mL) results in a reduction in the rate of growth but no bactericidal phase on Pseudomonas aeruginosa. Azlocillin decreases an initial lag phase with increasing drug concentration. At the lower concentration of tobramycin (0.5 μg/ml), the combinations with both the high and the low concentrations of Azlocillin are more effective than the individual components on Pseudomonas aeruginosa [3]. Isolates with derepression of AmpC enzyme are one to two doubling dilutions more resistant to azlocillin than are those in which increased efflux or impermeability is inferred. Those with secondary β-lactamases are mostly (12/14 cases) susceptible to ceftazidime at 4 mg/L, but are amongst the most resistant to Azlocillin (MIC ≥128 mg/L in 10/14 cases) [4].
Aztreonam is a synthetic monocyclic beta-lactam antibiotic, which has a very high affinity for penicillin-binding protein 3 (PBP-3).
Target: Penicillin-binding proteins 3 (PBP-3)
Aztreonam is a synthetic monocyclic beta-lactam antibiotic (a monobactam), with the nucleus based on a simpler monobactam isolated from Chromobacterium violaceum. It was approved by the U.S. Food and Drug Administration in 1986. It is resistant to some beta-lactamases, but is inactivated by extended-spectrum beta-lactamases. Aztreonam has no useful activity against gram-positive or anaerobic microorganisms
Aztreonam is similar in action to penicillin. It inhibits mucopeptide synthesis in the bacterial cell wall, thereby blocking peptidoglycan crosslinking. It has a very high affinity for penicillin-binding protein 3 (PBP-3) and mild affinity for PBP-1a. Aztreonam binds the penicillin-binding proteins of gram-positive and anaerobic bacteria very poorly and is largely ineffective against them. Aztreonam is bactericidal but less so than some of the cephalosporins
Bacitracin Zinc is a dephosphorylation of the C55-isoprenyl pyrophosphate interference for inhibition of cleavage of Tyr from Met-enkephalin with IC50 of 10 μM.
Target: Antibacterial
Bacitracin is a mixture of related cyclic polypeptides produced by organisms of the licheniformis group of Bacillus subtilis var Tracy. Its unique name derives from the fact that the bacillus producing it was first isolated in 1943 from a knee scrape from a girl named Margaret Tracy. As a toxic and difficult-to-use antibiotic, bacitracin doesn't work well orally. However, it is very effective topically. Bacitracin is synthesised via the so-called nonribosomal peptide synthetases (NRPSs), which means that ribosomes are not involved in its synthesis [1, 2].
Balofloxacin is quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase.
Target: Antibacterial; DNA gyrase.
Balofloxacin, an orally active fluoroquinolone antibiotic, has been developed by Choongwae Pharma in Korea, for the treatment of urinary tract infection (UTI). Chugai and Ciba were developing balofloxacin for respiratory tract infections (RTI) but discontinued development in 1995 due to changes in Chugai's R&D focus and a lack of efficacy of the drug. Following phase II trials, Choongwae bought the rights to develop balofloxacin in Korea from Chugai. Phase III trials for UTI were completed in early 2001. Balofloxacin was approved by the Korean FDA in December 2001 for UTI. In March 2002, phase II trials were underway for RTI.
Bedaquiline(TMC207; R207910) is an anti-tuberculosis drug which selectively inhibit the mycobacterial energy metabolism i.e. ATP synthesis and found to be effective against all states of Mycobacterium tuberculosis.
IC50 value:
Target: anti-TB
Preclinical studies have shown the efficacy of bedaquiline in terms of reduction in bacterial load and treatment duration. Phase II clinical studies have established the safety, tolerability and earlier sputum conversion time in patients with MDR-TB. In 2012 FDA approved bedaquiline for treatment of MDR-TB and XDR-TB [1]. Bedaquiline possesses a unique mechanism of action that disrupts the activity of the mycobacterial adenosine triphosphate synthase. Clinical trials have been conducted evaluating the use of bedaquiline in combination with a background regimen for the treatment of adults with pulmonary MDR-TB. Bedaquiline has an excellent in vitro activity against Mycobacterium tuberculosis, including multidrug resistant M tuberculosis; however, its side effect profile limits its use against MDR-TB when no other effective regimen can be provided [2].
Bedaquiline fumarate(TMC207; R207910) is an anti-tuberculosis drug which selectively inhibit the mycobacterial energy metabolism i.e. ATP synthesis and found to be effective against all states of Mycobacterium tuberculosis.
IC50 value:
Target: anti-TB
Preclinical studies have shown the efficacy of bedaquiline in terms of reduction in bacterial load and treatment duration. Phase II clinical studies have established the safety, tolerability and earlier sputum conversion time in patients with MDR-TB. In 2012 FDA approved bedaquiline for treatment of MDR-TB and XDR-TB [1]. Bedaquiline possesses a unique mechanism of action that disrupts the activity of the mycobacterial adenosine triphosphate synthase. Clinical trials have been conducted evaluating the use of bedaquiline in combination with a background regimen for the treatment of adults with pulmonary MDR-TB. Bedaquiline has an excellent in vitro activity against Mycobacterium tuberculosis, including multidrug resistant M tuberculosis; however, its side effect profile limits its use against MDR-TB when no other effective regimen can be provided [2].
Besifloxacin hydrochloride is a fourth-generation fluoroquinolone antibiotic.
IC50 Value:
Target: Antibacterial
Besifloxacin has been found to inhibit production of pro-inflammatory cytokines in vitro. Besifloxacin is a novel 8-chloro-fluoroquinolone agent with potent, bactericidal activity against prevalent and drug-resistant pathogens.besifloxacin is the most potent agent tested against gram-positive pathogens and anaerobes and is generally equivalent to comparator fluoroquinolones in activity against most gram-negative pathogens. Besifloxacin demonstrates potent, broad-spectrum activity, which is particularly notable against gram-positive and gram-negative isolates that are resistant to other fluoroquinolones and classes of antibacterial agents.
Betulinaldehyde(Betunal) belongs to pentacyclic triterpenoids and was reported to exhibit antimicrobial activities against bacteria and fungi, including S. aureus.
IC50 value:
Target:
Betulinaldehyde(Betunal) belongs to pentacyclic triterpenoids that are based on a 30-carbon skeleton comprising four six-membered rings and one five-membered ring. Betulinaldehyde regulates multiple desirable targets which could be further explored in the development of therapeutic agents for the treatment of S. aureus infections [1]. Study compounds α-amyrin [3β-hydroxy-urs-12-en-3-ol (AM)], betulinic acid [3β-hydroxy-20(29)-lupaene-28-oic acid (BA)] and betulinaldehyde [3β-hydroxy-20(29)-lupen-28-al (BE)] belong to pentacyclic triterpenoids and were reported to exhibit antimicrobial activities against bacteria and fungi, including S. aureus. The MIC values of these compounds against a reference strain of methicillin-resistant S. aureus (MRSA) (ATCC 43300) ranged from 64 μg/ml to 512 μg/ml. However, the response mechanisms of S. aureus to these compounds are still poorly understood [2].
Biapenem is a parenteral carbapenem antibacterial agent with a broad spectrum.
Target: Antibacterial
Biapenem is a carbapenem antibiotic of in vitro antibacterial activity encompassing many Gramnegative and Gram-positive aerobic and anaerobic bacteria, including species producing β-lactamases. Biapenem is more stable than imipenem, mero-penem and panipenem to hydrolysis by human renal dihydropeptidase-I (DHP-I), and therefore does not require the coadministration of a DHP-I inhibitor. In randomised, nonblind or double-blind clinical trials, biapenem showed good clinical and bacteriological efficacy (similar to that of imipenem/ cilastatin) in the treatment of adult patients with intra-abdominal infections, lower respiratory infections or complicated urinary tract infections.
Capreomycin is a peptide antibiotic, commonly grouped with the aminoglycosides, which is given in combination with other antibiotics for MDR-tuberculosis.
IC50 value:
Target:
The drug should not be given with streptomycin or other drugs that may damage the auditory vestibular nerve. Patients on this drug will often require audiology tests. It is a cyclic peptide.Capreomycin is administered intramuscularly and shows bacteriostatic activity.
Carbenicillin is broad-spectrum semisynthetic penicillin derivative used parenterally.
Target: Antibacterial
Carbenicillin is a semi-synthetic penicillin antibiotic which interferes with cell wall synthesis of gram-negative bacteria while displaying low toxicity. The leukocytes of the patients does not release histamine on in vitro provocation with Carbenicillin (0.1 g/mL). Carbenicillin (0.1 g/mL) does not show any allergic drug reactions in cystic fibrosis patients, as evident by no significant levels of antibodies of IgE, IgG or IgM classes [1]. Carbenicillin (50 μg/mL) results in phytotoxicity in chrysanthemum and TOB, with an increase in the concentration, and with a parallel shift in the morphogenic capacity (SRC) of threshold survival levels (TSLs). Carbenicillin results in 100% acclimatization with no different morphological flowering characteristics following subculture in vitro three times in Chrysanthemum plantlets [2].
Carbenicillin Disodium is a broad-spectrum semisynthetic penicillin derivative used parenterally.
Target: Antibacterial
Carbenicillin is a semi-synthetic penicillin antibiotic which interferes with cell wall synthesis of gram-negative bacteria while displaying low toxicity. The leukocytes of the patients does not release histamine on in vitro provocation with Carbenicillin (0.1 g/mL). Carbenicillin (0.1 g/mL) does not show any allergic drug reactions in cystic fibrosis patients, as evident by no significant levels of antibodies of IgE, IgG or IgM classes [1]. Carbenicillin (50 μg/mL) results in phytotoxicity in chrysanthemum and TOB, with an increase in the concentration, and with a parallel shift in the morphogenic capacity (SRC) of threshold survival levels (TSLs). Carbenicillin results in 100% acclimatization with no different morphological flowering characteristics following subculture in vitro three times in Chrysanthemum plantlets [2].
Cefaclor, is a second-generation cephalosporin antibiotic used to treat certain infections caused by bacteria such as pneumonia and infections of the ear, lung, skin, throat, and urinary tract.
Target: Antibacterial
Cefaclor belongs to the family of antibiotics known as the cephalosporins (cefalosporins). The cephalosporins are broad-spectrum antibiotics that are used for the treatment of septicaemia, pneumonia, meningitis, biliary tract infections, peritonitis, and urinary tract infections. The pharmacology of the cephalosporins is similar to that of the penicillins, excretion being principally renal. Cephalosporins penetrate the cerebrospinal fluid poorly unless the meninges are inflamed; cefotaxime is a more suitable cephalosporin than cefaclor for infections of the central nervous system, e.g. meningitis. Cefaclor is active against many bacteria, including both Gram-negative and Gram-positive organisms.
Cefaclor is frequently used against bacteria responsible for causing skin infections, otitis media, urinary tract infections, and others. The following represents MIC susceptibility data for a few medically significant microorganisms. Cefaclor is passed into the breast milk in small quantities, but is generally accepted to be safe to take during breastfeeding. Cefaclor is not known to be harmful in pregnancy. Cefaclor has also been reported to cause a serum sickness-like reaction in children.
Cefdinir (Omnicef) is a semi-synthetic, broad-spectrum antibiotic, which is proved to be effective for common bacterial infections of the ear, sinus, throat, and skin.
Target: Antibacterial
Cefdinir is a third generation oral cephalosporin antibiotic. Cefdinir (Omnicef) is a semi-synthetic, broad-spectrum antibiotic in the third generation of the cephalosporin class, which is proved to be effective for common bacterial infections of the ear, sinus, throat, and skin. It can be used to treat infections caused by several Gram-negative and Gram-positive bacteria. It is available in US as Omnicef by Abbott Laboratories and in India as Cednir by Abbott, Kefnir by Glenmark and Cefdiel by Ranbaxy. As of 2008, cefdinir was the highest-selling cephalosporin antibiotic in the United States, with more than US$585 million in retail sales of its generic versions alone.
Cefdinir, a new oral 2-amino-5-thiazolyl cephalosporin, inhibited the luminol-amplified chemiluminescence (LACL) response of human neutrophils stimulated by PMA but not opsonized zymosan, in a concentration-dependent but not time-dependent manner. The LACL response to opsonized zymosan in cytochalasin B-treated neutrophils was, however, inhibited by cefdinir. Furthermore, cefdinir inhibited LACL generation in cell-free systems consisting of H2O2, NaI, and either horseradish peroxidase or a myeloperoxidase-containing neutrophil extract. Orthodianisidine oxidation in these two acellular systems was inhibited by cefdinir.
Cefditoren pivoxil is a new-third generation cephalosporin antibiotic that has a broad spectrum of activity against Gram-positive and Gram-negative bacteria, including common respiratory and skin pathogens.
Target: Antibacterial
Cefditoren pivoxil, a new-third generation cephalosporin antibiotic that has recently been granted approval in Spain, shows important activity over a large part of the pathogens causing skin, soft tissue and respiratory tract infections, including Gram-negative and Gram-positive bacteria. Cefditoren is also marketed under the name Meiact. Cefditoren has a broad spectrum of activity and has been used to treat bacterial infections of the skin and respiratory tract including bronchitis, pneumonia, and tonsillitis. The following represents MIC susceptibility data for a few medically significant microorganisms.
Cefditoren has shown excellent in vitro activity against the Gram-positive pathogens penicillin-susceptible and -intermediate Streptococcus pneumoniae, S. pyogenes and methicillin-susceptible Staphylococcus aureus. Cefditoren was inactive against methicillin-resistant S. aureus. Of the important Gram-negative pathogens, cefditoren had potent antibacterial effects against beta-lactamase-positive and -negative Haemophilus influenzae, H. parainfluenzae and beta-lactamase-positive and -negative Moraxella catarrhalis.
Cefepime Dihydrochloride Monohydrate is a broad-spectrum cephalosporin with enhanced coverage against Gram-positive and Gram-negative bacteria.
Target: Antibacterial
Cefepime is an extended-spectrum parenteral cephalosporin antibiotic active in vitro against a broad spectrum of gram-positive and gram-negative aerobic bacteria. Cefepime dosing was 1-4 g/day (0.5-2.0 g twice daily) for adults; ceftazidime dosing was 1-6 g/day (0.5 g every 12 hours to 2.0 g every 8 hours). A limited number of cefepime-treated patients received 2 g every 8 hours. The median length of dosing for both cefepime and ceftazidime was 7 days [1]. Cefepime has a decreased propensity to induce beta-lactamases compared with other beta-lactam antibiotics. Cefepime has a pharmacokinetic disposition similar to that of other renally eliminated cephalosporins, with a half-life of approximately 2 hours. Cefepime has demonstrated clinical efficacy against a variety of infections, including urinary tract infections, pneumonia, and skin and skin structure infections. Cefepime is generally well tolerated [2].
Cefoperazone is a cephalosporin antibiotic for inhibition of rMrp2-mediated [3H]E217βG uptake with IC50 of 199 μM.
Target: Antibacterial
Cefoperazone is a sterile, semisynthetic, broad-spectrum, parenteral cephalosporin antibiotic for intravenous or intramuscular administration. After intravenous administration of 2 g of Cefoperazone, levels in serum rang from 202μg/mL to 375 μg/mL depending on the period of drug administration. After intramuscular injection of 2 g of Cefoperazone, the mean peak serum level is 111 μg/mL at 1.5 hours. At 12 hours after dosing, mean serum levels are still 2 to 4 μg/mL. Cefoperazone is 90% bound to serum proteins.
Cefoselis is a widely used beta-lactam antibiotic.
Target: Antibacterial
Cefoselis, a new parenteral cephalosporin, was active against clinical isolates of both gram-positive and gram-negative aerobic bacteria. The activity of Cefoselis was similar to that of cefpirome and cefepime and generally superior to that of ceftazidime. Cefoselis showed potent antibacterial activity against Hemophilus influenzae and Moraxella catarrhalis.Cefoselis was highly active against MSSA and MSCNS. Cefoselis was poor in the activity against MRSA,MRCNS,PRSP and Enterococcus faecalis,and no activity for Enterococcus faecium.
Cefoselis is a widely used beta-lactam antibiotic.
Target: Antibacterial
Cefoselis, a new parenteral cephalosporin, was active against clinical isolates of both gram-positive and gram-negative aerobic bacteria. The activity of Cefoselis was similar to that of cefpirome and cefepime and generally superior to that of ceftazidime. Cefoselis showed potent antibacterial activity against Hemophilus influenzae and Moraxella catarrhalis.Cefoselis was highly active against MSSA and MSCNS. Cefoselis was poor in the activity against MRSA,MRCNS,PRSP and Enterococcus faecalis,and no activity for Enterococcus faecium.
Cefoselis is a widely used beta-lactam antibiotic.
Target: Antibacterial
Cefoselis, a new parenteral cephalosporin, was active against clinical isolates of both gram-positive and gram-negative aerobic bacteria. The activity of Cefoselis was similar to that of cefpirome and cefepime and generally superior to that of ceftazidime. Cefoselis showed potent antibacterial activity against Hemophilus influenzae and Moraxella catarrhalis.Cefoselis was highly active against MSSA and MSCNS. Cefoselis was poor in the activity against MRSA,MRCNS,PRSP and Enterococcus faecalis,and no activity for Enterococcus faecium.
Cefozopran(SCE 2787) is a fourth-generation cephalosporin.
Target: Antibacterial
Cefozopran is a fourth-generation cephalosporin.
Cefozopran Hcl(SCE 2787 Hcl) is a fourth-generation cephalosporin.
Target: Antibacterial
Cefozopran is a fourth-generation cephalosporin.
Cefprozil Monohydrate (Cefzil) is a second-generation cephalosporin type antibiotic.
Target: Antibacterial
Cefprozil, sometimes spelled cefproxil and marketed under the trade name Cefzil, is a second-generation cephalosporin type antibiotic. In Europe it is marketed using the trade names Procef and Cronocef. It can be used to treat bronchitis, ear infections, skin infections, and other bacterial infections. It comes as a tablet and as a liquid suspension. From Wikipedia.
Ceftazidime(GR20263) is an antibiotic useful for the treatment of a number of bacterial infections.
Target: Antibacterial
Ceftazidime is an antibiotic useful for the treatment of a number of bacterial infections. It is a third-generation cephalosporin. As with all antibiotics, ceftazidime is not used to treat viral infections. Cephalosporins have activity against Gram-positive and Gram-negative bacteria. The balance of activity tips toward Gram-positive organisms for earlier generations; later generations of cephalosporins have more Gram-negative coverage. Ceftazidime is one of the few in this class with activity against Pseudomonas. It is not active against Methicillin-resistant Staphylococcus aureus. From Wikipedia.
Ceftibuten(Sch39720) is a third-generation cephalosporin antibiotic.
Target: Antibacterial
Ceftibuten displayed high activity against Haemophilus influenzae and Branhamella catarrhalis. There was reduced activity against Streptococcus pneumoniae (MIC90 16 mg/l). The protein binding of ceftibuten was 77% and the primary target site PBP 3. A high degree of stability to beta-lactamase hydrolysis was observed [1].
Ceftriaxone is an antibiotic useful for the treatment of a number of bacterial infections.
Target: Antibacterial
Ceftriaxone inhibits bacterial cell wall synthesis by means of binding to the penicillin-binding proteins (PBPs). Inhibition of PBPs would in turn inhibit the transpeptidation step in peptidoglycan synthesis which is required for bacterial cell walls. Like other cephalosporins, ceftriaxone is bacteriocidal and exhibits time-dependent killing. Ceftriaxone, one of the beta-lactam antibiotics, is a stimulator of EAAT2 expression with neuroprotective effects in both in vitro and in vivo models based in part on its ability to inhibit neuronal cell death by glutamate excitotoxicity. Based on this consideration and its lack of toxicity, ceftriaxone has potential to manipulate glutamate transmission and ameliorate neurotoxicity [1].
Cefalexin is a cephalosporin antibiotic.
Target: Antibacterial
Cefalexin (INN, BAN) or cephalexin (USAN, AAN) is a first-generation cephalosporin antibiotic introduced in 1967 by Eli Lilly and Company. It is an orally administered agent with a similar antimicrobial spectrum to the intravenous agents cefalotin and cefazolin. It was first marketed as Keflex (Lilly), and is marketed under several other trade names. As of 2008, cefalexin was the most popular cephalosporin antibiotic in the United States, with more than 25 million prescriptions of its generic versions alone, for US$255 million in sales (though less popular than two other antibiotics, amoxicillin and azithromycin, each with 50 million prescriptions per year).
Cefalexin is marketed by generic pharmaceutical manufacturers under a wide range of brand names, including: Apo-Cephalex, Biocef, Cefanox, Ceforal, Cephabos, Cephalexin, Cephorum, Ceporex, Cilex, Ialex, Ibilex, Kefexin, Keflet, Keflex, Rekosporin, Keforal, Keftab, Keftal, Lopilexin, Larixin, Novo-Lexin, Ospexin, Tenkorex, Zephalexin, Panixine Disperdose, Rancef, Sialexin, Sporidex and Ulexin. A version of Keflex 750 mg capsules is marketed for twice-daily dosage, to improve compliance. However, it is not a sustained release formulation, and since it is more expensive than the older strengths, some physicians prescribe three 250 mg capsules to be taken twice daily, as a less expensive alternative.
Cefalexin hydrochloride is a cephalosporin antibiotic.
Target: Antibacterial
Cefalexin (INN, BAN) or cephalexin (USAN, AAN) is a first-generation cephalosporin antibiotic introduced in 1967 by Eli Lilly and Company. It is an orally administered agent with a similar antimicrobial spectrum to the intravenous agents cefalotin and cefazolin. It was first marketed as Keflex (Lilly), and is marketed under several other trade names. As of 2008, cefalexin was the most popular cephalosporin antibiotic in the United States, with more than 25 million prescriptions of its generic versions alone, for US$255 million in sales (though less popular than two other antibiotics, amoxicillin and azithromycin, each with 50 million prescriptions per year).
Cefalexin is marketed by generic pharmaceutical manufacturers under a wide range of brand names, including: Apo-Cephalex, Biocef, Cefanox, Ceforal, Cephabos, Cephalexin, Cephorum, Ceporex, Cilex, Ialex, Ibilex, Kefexin, Keflet, Keflex, Rekosporin, Keforal, Keftab, Keftal, Lopilexin, Larixin, Novo-Lexin, Ospexin, Tenkorex, Zephalexin, Panixine Disperdose, Rancef, Sialexin, Sporidex and Ulexin. A version of Keflex 750 mg capsules is marketed for twice-daily dosage, to improve compliance. However, it is not a sustained release formulation, and since it is more expensive than the older strengths, some physicians prescribe three 250 mg capsules to be taken twice daily, as a less expensive alternative.
Cefalexin monohydrate is a cephalosporin antibiotic.
Target: Antibacterial
Cefalexin (INN, BAN) or cephalexin (USAN, AAN) is a first-generation cephalosporin antibiotic introduced in 1967 by Eli Lilly and Company. It is an orally administered agent with a similar antimicrobial spectrum to the intravenous agents cefalotin and cefazolin. It was first marketed as Keflex (Lilly), and is marketed under several other trade names. As of 2008, cefalexin was the most popular cephalosporin antibiotic in the United States, with more than 25 million prescriptions of its generic versions alone, for US$255 million in sales (though less popular than two other antibiotics, amoxicillin and azithromycin, each with 50 million prescriptions per year).
Cefalexin is marketed by generic pharmaceutical manufacturers under a wide range of brand names, including: Apo-Cephalex, Biocef, Cefanox, Ceforal, Cephabos, Cephalexin, Cephorum, Ceporex, Cilex, Ialex, Ibilex, Kefexin, Keflet, Keflex, Rekosporin, Keforal, Keftab, Keftal, Lopilexin, Larixin, Novo-Lexin, Ospexin, Tenkorex, Zephalexin, Panixine Disperdose, Rancef, Sialexin, Sporidex and Ulexin. A version of Keflex 750 mg capsules is marketed for twice-daily dosage, to improve compliance. However, it is not a sustained release formulation, and since it is more expensive than the older strengths, some physicians prescribe three 250 mg capsules to be taken twice daily, as a less expensive alternative.
CHIR-090 is a potent LpxC inhibitor, displays two-step time-dependent inhibition and kills a wide range of Gram-negative pathogens as effectively as ciprofloxacin or tobramycin.
IC50 value:
Target: LpxC; Antibacterial; LpxC
The UDP-3-O-(R-3-hydroxyacyl)-N-acetylglucosamine deacetylase LpxC is an essential enzyme of lipid A biosynthesis in Gram-negative bacteria and a promising antibiotic target.
Chloramphenicol is a broad-spectrum antibiotic.
Target: Antibacterial
Chloramphenicol is a bacteriostatic drug that stops bacterial growth by inhibiting protein synthesis. Chloramphenicol prevents protein chain elongation by inhibiting the peptidyl transferase activity of the bacterial ribosome. It specifically binds to A2451 and A2452 residues in the 23S rRNA of the 50S ribosomal subunit, preventing peptide bond formation. While chloramphenicol and the macrolide class of antibiotics both interact with ribosomes, chloramphenicol is not a macrolide. It directly interferes with substrate binding, whereas macrolides sterically block the progression of the growing peptide [1, 2].
Chlorhexidine is an antiseptic effective against a wide variety of gram-negative and gram-positive organisms.
Target: Antibacterial
Chlorhexidine is a chemical antiseptic.It is effective on both Gram-positive and Gram-negative bacteria, although it is less effective with some Gram-negative bacteria.It has both bactericidal and bacteriostatic mechanisms of action, the mechanism of action being membrane disruption, not ATPase inactivation as previously thought.It is also useful against fungi and enveloped viruses, though this has not been extensively investigated. Chlorhexidine is harmful in high concentrations, but is used safely in low concentrations in many products, such as mouthwash and contact lens solutions [1, 2].
Chloroxine is a synthetic antibacterial compound that is effective in the treatment of dandruff and seborrheic dermatitis when incorporated in a shampoo.
Target: Antibacterial
Chloroxine is an antibacterial drug. Oral formulations are used in infectious diarrhea, disorders of the intestinal microflora (e.g. after antibiotic treatment), giardiasis, inflammatory bowel disease. It is also useful for dandruff and seborrheic dermatitis, as used in shampoos and dermal creams like. Chloroxine has bacteriostatic, fungistatic and antiprotozoal properties. It is effective against Streptococci, Staphylococci, Candida, Candida albicans, Shigella and Trichomonads.
Ciprofloxacin is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity.
Target: Antibacterial
Ciprofloxacin is a fluoroquinolone antibiotic, shows MIC90 (minimal inhibitory concentrations for 90%) of between 0.008 and 2 μg/ml for Enterobacteriaceae, Pseudomonas aeruginosa, Haemophilus influenzae, Neisseria gonorrhoeae, streptococci, Staphylococcus aureus, and Bacteroidesfragilis strains [1]. Ciprofloxacin inhibits topoisomerase IV as a primary topoisomerase target and gyrase as a secondary target [2]. Ciprofloxacin shows an AUC (area under the curve) of 24 μg×h/ml [3].
Clarithromycin is a macrolide antibiotic and a CYP3A4 inhibitor.
Target: Antibacterial; CYP3A4
Clarithromycin is a macrolide antibiotic used to treat pharyngitis, tonsillitis, acute maxillary sinusitis, acute bacterial exacerbation of chronic bronchitis, pneumonia (especially atypical pneumonias associated with Chlamydophila pneumoniae), skin and skin structure infections. Clarithromycin prevents bacteria from growing by interfering with their protein synthesis. It binds to the subunit 50S of the bacterial ribosome and thus inhibits the translation of peptides. Clarithromycin has similar antimicrobial spectrum as erythromycin, but is more effective against certain Gram-negative bacteria, particularly Legionella pneumophila. Besides this bacteriostatic effect, clarithromycin also has bactericidal effect on certain strains, such as Haemophilus influenzae, Streptococcus pneumoniae and Neisseria gonorrhoeae. Clarithromycin is a CYP3A4 inhibitor. Even low doses of the cytochrome P4503A4 (CYP3A4) inhibitor clarithromycin increase the plasma concentrations and effects of repaglinide. Concomitant use of clarithromycin or other potent inhibitors of CYP3A4 with repaglinide may enhance its blood glucose-lowering effect and increase the risk of hypoglycemia [1, 2].
Clinafloxacin(PD-127391) is a fluoroquinolone antibiotic.
Target: Antibacterial
Clinafloxacin is a broad-spectrum antibiotic of the quinolone carboxylic acid category currently in development for intravenous and oral therapy of serious infections [1]. Clinafloxacin is a novel fluoroquinolone with potent broad-spectrum in vitro activity against gram-positive, gram-negative, and anaerobic pathogens. Clinafloxacin is highly active against S. pneumoniae 7785 (MIC, 0.125 μg/mL), and neither gyrA nor parC quinolone resistance mutations alone have much effect on this activity [2]. Clinafloxacin is identified as the most active fluoroquinolone against S. pneumoniae when compared with ofloxacin, levofloxacin, sparfloxacin, grepafloxacin, and trovafloxacin and is currently being evaluated as an antipneumococcal agent [3].
Clindamycin Hydrochloride is a semisynthetic lincosamide antibiotic.
Target: Antibacterial
Clindamycin is a lincosamide antibiotic. It is usually used to treat infections with anaerobic bacteria, but can also be used to treat some protozoal diseases, such as malaria. It is a common topical treatment for acne and can be useful against some methicillin-resistant Staphylococcus aureus (MRSA) infections [1]. Clindamycin is rapidly accumulated by polymorphonuclear neutrophils(PMNs), that drug uptake is related to a pH gradient, and that clindamycin appears to be lysosomotropic [2].
Cloxacillin sodium monohydrate is a semi-synthetic antibiotic that is a chlorinated derivative of oxacillin.
Target: Antibacterial
Cloxacillin sodium (Cloxacap) is a sodium salt of cloxacillin that is a penicillinase-resistant, acid resistant, semi-synthetic penicillin. Cloxacillin sodium exerts a bactericidal action against susceptible microorganisms during the stage of active multiplication. Cloxacillin sodium acts through the inhibition of biosynthesis of cell wall mucopeptides. Cloxacillin sodium is readily absorbed following i.m. administration and rapidly reaches therapeutically effective blood levels. Serum levels are approximately proportional to dosage. Peak plasma concentrations of 15 ug/ml have been observed 30 minutes after an i.m. injection of cloxacillin (Cloxapen, Cloxacap and Orbenin) 500 mg; plasma concentrations may be doubled by administration of a doubled dose. At the end of a 3-hour i.v. infusion of cloxacillin (Cloxapen, Cloxacap and Orbenin) 250 mg given to normal subjects, its plasma concentrations were 15 ug/ml. After 2 hours, plasma concentrations were 0.6 ug/ml [1].
D-Cycloserine is an analog of the amino acid D-alanine.
Target: Antibacterial
D-Cycloserine selectively potentiated the duration of motor cortical excitability enhancements induced by anodal tDCS. D-Cycloserine alone did not modulate excitability [1]. Participants receiving d-cycloserine in addition to exposure therapy reported significantly less social anxiety compared with patients receiving exposure therapy plus placebo. Controlled effect sizes were in the medium to large range [2]. Chronic D-cycloserine significantly reduced nicotine self-administration selectively in rats with low baseline nicotine use, but was ineffective with the rats with higher levels of baseline nicotine self-administration [3].
Dalbavancin(BI-397; MDL-63397) is a semisynthetic lipoglycopeptide, has potent activity against Gram-positive bacteria(MIC50=0.06 mg/L; B. anthracis).
IC50 value: 0.06 mg/L(MIC50; B. anthracis) [1]
Target: Antibiotic
Dalbavancin demonstrated potent in vitro activity against B. anthracis (MIC range, < or =0.03 to 0.5 mg/liter; MIC(50) and MIC(90), 0.06 and 0.25 mg/liter, respectively), which led us to test its efficacy in a murine inhalation anthrax model. At 20 mg/kg, the dalbavancin activity was detectable for 6 days after administration (terminal half-life, 53 h), indicating that long intervals between doses were feasible. The mice were challenged with 50 to 100 times the median lethal dose of the Ames strain of B. anthracis, an inoculum that kills untreated animals within 4 days. The efficacy of dalbavancin was 80 to 100%, as determined by the rate of survival at 42 days, when treatment was initiated 24 h postchallenge with regimens of 15 to 120 mg/kg every 36 h (q36h) or 30 to 240 mg/kg every 72 h (q72h). A regimen of ciprofloxacin known to protect 100% of animals was tested in parallel. Delayed dalbavancin treatment (beginning 36 or 48 h postchallenge) with 60 mg/kg q36h or 120 mg/kg q72h still provided 70 to 100% survival [1]. Dalbavancin features a multifaceted mechanism of action that inhibits bacterial cell wall formation by two different mechanisms that enhances its activity against a wide range of gram-positive bacteria including staphylococci, streptococci, enterococci, and some anaerobes. Additionally, dalbavancin possesses unique pharmacokinetic properties, the most significant of which is a long terminal half-life that allows for once weekly dosing [2].
Danofloxacin Mesylate(CP76136-27 mesylate) is a fluoroquinolone antibacterial for veterinary use.
Target: Antibacterial
Danofloxacin is a synthetic antibacterial agent of the fluoroquinolone class, acts principally by the inhibition of bacterial DNA-gyrase, which is necessary for supercoiling of DNA to provide a suitable spatial arrangement of DNA within the bacterial cell. The minimum inhibitory concentration of danofloxacin against 90% (MIC90) of contemporary European and North American field isolates of Pasteurella haemolytica, Pasteurella multocida and Haemophilus somnus, the most important bacterial respiratory pathogens of cattle, is 0.125 μg/ml [1]. Danofloxacin shows protective dose (PD50) of 0.38, 0.8, 2.42 mg/kg for P. multocida, E. coli and S. choleraesuis in in vivo mouse protection assay [2].
Dapsone is a sulfone active against a wide range of bacteria but mainly employed for its actions against mycobacterium leprae.
Target: Antibacterial
Dapsone is an antibacterial most commonly used in combination with rifampicin and clofazimine as multidrug therapy (MDT) for the treatment of Mycobacterium leprae infections (leprosy). Dapsone antagonized all of the I/R end points measured, showing a remarkable ability to decrease markers of damage through antioxidant, antiinflammatory, and anti-apoptotic effects [1]. As an antibacterial, dapsone inhibits bacterial synthesis of dihydrofolic acid, via competition with para-aminobenzoate for the active site of dihydropteroate synthetase. Dapsone has anti-inflammatory and immunomodulatory effects [2].
Daptomycin is a novel lipopeptide antimicrobial agent with activity against Gram-positive organisms, including multi-resistant strains.
Target: Antibacterial
Daptomycin is a novel lipopeptide antibiotic used in the treatment of certain infections caused by Gram-positive organisms. It is a naturally-occurring compound found in the soil saprotroph Streptomyces roseosporus. Its distinct mechanism of action means that it may be useful in treating infections due to Staphylococcus aureus [1].
The efficacies of low- versus high-dose vancomycin (10 versus 110 mg/kg), daptomycin (1 versus 10 mg/kg), and tigecycline (1 versus 10 mg/kg) intravenous prophylaxis were compared using in vivo bioluminescence imaging, ex vivo bacterial counts, and biofilm formation. High-dose vancomycin, daptomycin, and tigecycline resulted in similar reductions in bacterial burden and biofilm formation. In contrast, low-dose daptomycinand tigecycline were more effective than low-dose vancomycin against the implant infection. In this mouse model of surgical implant MSSA or MRSA infection, daptomycin and tigecycline prophylaxis were effective over a broader dosage range than vancomycin [2].
Clinical indications: Bacterial endocarditis; Bacterial infection; Bacterial skin infection; Enterococcus faecalis infection; Gram positive bacterium infection; MRSA infection; Osteomyelitis; Sepsis; Staphylococcus aureus infection; Streptococcus agalactiae infection; Streptococcus infection; Streptococcus pyogenes infection
FDA Approved Date: September 2003
Toxicity: hypotension; headache; insomnia; rash; constipation; nausea; diarrhea
Demeclocycline Hcl is a tetracycline antibiotic; is an antibiotic in the treatment of Lyme disease, acne, and bronchitis.
Dirithromycin(LY 237216) is a macrolide glycopeptide antibiotic by binding to the 50S subunit of the 70S bacterial ribosome to inhibit the translocation of peptides.
Target: Antibacterial
Dirithromycin is a new macrolide with a spectrum and degree of in vitro antimicrobial activity similar to that of erythromycin. Compared with erythromycin, dirithromycin has a long elimination half-life enabling once-daily administration, and it also achieves a greater cellular:extracellular concentration ratio and higher concentration in some tissues. Multicentre double-blind clinical trials have shown dirithromycin to be similar in efficacy to erythromycin in the treatment of uncomplicated bacterial infections of the respiratory tract and of skin and soft tissues [1]. Dirithromycin offers some attractive pharmacokinetic properties. The long elimination half-life of dirithromycin allows once-daily dosing and higher and more prolonged tissue concentrations than are achievable with erythromycin. The spectrum of activity, adverse effect profile, clinical efficacy, and bacteriologic eradication rate of dirithromycin may be similar to those of erythromycin [2, 3].
Doripenem is a new member of the carbapenem class of beta-lactam antibiotics with broad-spectrum coverage of Gram-positive, Gram-negative and anaerobic pathogens.
Target: Antibacterial
Doripenem is an ultra-broad-spectrum injectable antibiotic. It is a beta-lactam and belongs to the subgroup of carbapenems. It was launched by Shionogi Co. of Japan under the brand name Finibax in 2005 and is being marketed outside Japan by Johnson & Johnson. It is particularly active against Pseudomonas aeruginosa. It is recommended that those allergic to doripenem or to any type of beta-lactam antibiotics such as cephalosporin or other Carbapenems not receive doripenem.
Doripenem appears as crystalline powder anywhere from a white to somewhat yellowish colour.Doripenem is moderately soluble in water, slightly soluble in methanol, and virtually insoluble in ethanol. Doripenem is also solution in N,N-dimethylformamide. Doripenem's chemical configuration has 6 asymmetrical carbon atoms (6 stereocentres) and is most commonly supplied as one pure isomer. In terms of doripenem for injection, the crystallized powered drug can form a monohydrate when mixed with water. However, Doripenem has not been proven to possess polymorphism.
Doripenem monohydrate is a new member of the carbapenem class of beta-lactam antibiotics with broad-spectrum coverage of Gram-positive, Gram-negative and anaerobic pathogens.
Target: Antibacterial
Doripenem is an ultra-broad-spectrum injectable antibiotic. It is a beta-lactam and belongs to the subgroup of carbapenems. It was launched by Shionogi Co. of Japan under the brand name Finibax in 2005 and is being marketed outside Japan by Johnson & Johnson. It is particularly active against Pseudomonas aeruginosa. It is recommended that those allergic to doripenem or to any type of beta-lactam antibiotics such as cephalosporin or other Carbapenems not receive doripenem.
Doripenem appears as crystalline powder anywhere from a white to somewhat yellowish colour.Doripenem is moderately soluble in water, slightly soluble in methanol, and virtually insoluble in ethanol. Doripenem is also solution in N,N-dimethylformamide. Doripenem's chemical configuration has 6 asymmetrical carbon atoms (6 stereocentres) and is most commonly supplied as one pure isomer. In terms of doripenem for injection, the crystallized powered drug can form a monohydrate when mixed with water. However, Doripenem has not been proven to possess polymorphism.
Doxycycline Hyclate is a synthetic tetracycline derivative with similar antimicrobial activity.
Target: Antibacterial
Doxycycline is a tetracycline antibiotic which is commonly used to treat a variety of infections. Doxycycline treatment resulted in a 96% loss of Wolbachia, as determined by real time PCR from microfilariae. The mechanism of doxycycline is similar to that in other filarial species, i.e., a predominant blockade of embryogenesis, leading to a decline of microfilariae according to their half-life [1]. Doxycycline treatment inhibits the activity of tissue MMP and attenuates the decrease in the collagen content in aortas of mice haploinsufficient for collagen III, as well as prevents the development of stress-induced vessel pathology. The results suggest that doxycycline merits clinical testing as a treatment for vEDS [2]. One person from the doxycycline group died from HIV infection. Five (doxycycline) and 11 (placebo) individuals were absent at the time of ultrasound analysis. Doxycycline treatment almost completely eliminated microfilaraemia at 8-14 months' follow-up (for all timepoints p<0.001). Ultrasonography detected adult worms in only six (22%) of 27 individuals treated with doxycycline compared with 24 (88%) of 27 with placebo at 14 months after the start of treatment (p<0.0001) [3].
Doxycycline Hydrochloride is a synthetic tetracycline derivative with similar antimicrobial activity.
Target: Antibacterial
Doxycycline is a tetracycline antibiotic which is commonly used to treat a variety of infections. Doxycycline treatment resulted in a 96% loss of Wolbachia, as determined by real time PCR from microfilariae. The mechanism of doxycycline is similar to that in other filarial species, i.e., a predominant blockade of embryogenesis, leading to a decline of microfilariae according to their half-life [1]. Doxycycline treatment inhibits the activity of tissue MMP and attenuates the decrease in the collagen content in aortas of mice haploinsufficient for collagen III, as well as prevents the development of stress-induced vessel pathology. The results suggest that doxycycline merits clinical testing as a treatment for vEDS [2]. One person from the doxycycline group died from HIV infection. Five (doxycycline) and 11 (placebo) individuals were absent at the time of ultrasound analysis. Doxycycline treatment almost completely eliminated microfilaraemia at 8-14 months' follow-up (for all timepoints p<0.001). Ultrasonography detected adult worms in only six (22%) of 27 individuals treated with doxycycline compared with 24 (88%) of 27 with placebo at 14 months after the start of treatment (p<0.0001) [3].
Enoxacin is a broad-spectrum 6-fluoronaphthyridinone antibacterial agent.
Target: antibacterial
Enoxacin is a new quinolone carboxylic acid compound. Its activity against 740 bacterial isolates was determined. It inhibited 90% Escherichia coli, Klebsiella sp., Aeromonas sp., Enterobacter spp., Serratia spp., Proteus mirabilis, and Morganella morganii at less than or equal to 0.8 micrograms/ml [1]. Daily plasma theophylline concentrations were measured in 14 patients. The mean +/- s.d. theophylline concentrations increased from 8.5 +/- 2.8 micrograms ml-1 prior to enoxacin to a maximum of 21.7 +/- 7.8 micrograms ml-1 during coadministration [2].
Enrofloxacin(BAY-Vp2674; PD160788) is a fluoroquinolone antibiotic.
Target: Antibacterial
Enrofloxacin is a fluoroquinolone antibiotic sold by the Bayer Corporation under the trade name Baytril. Enrofloxacin is currently approved by the FDA for the treatment of individual pets and domestic animals in the United States. Enrofloxacin is a bactericidal agent. The bactericidal activity of enrofloxacin is concentration-dependent, with susceptible bacteria cell death occurring within 20-30 minutes of exposure. Enrofloxacin has demonstrated a significant post-antibiotic effect for both Gram-negative and Gram-positive bacteria and is active in both stationary and growth phases of bacterial replication. Enrofloxacin has antibacterial activity against a broad spectrum of Gram-negative and Gram-positive bacteria. Its mechanism of action is not thoroughly understood, but it is believed to act by inhibiting bacterial DNA gyrase (a type-II topoisomerase), thereby preventing DNA supercoiling and DNA synthesis. From Wikipedia.
Eperezolid(PNU-100592) is a oxazolidinone antibacterial agent, Eperezolid demonstrated good in vitro inhibitory activity, regardless of methicillin susceptibility for staphylococci(MIC90= 1-4 mg/ml).
IC50 value: 1-4 mg/ml (MIC90, staphylococci) [1]
Target: Antibiotic
Eperezolid binds specifically to the 50S ribosomal subunit of Escherichia coli. The specific binding of eperezolid is dose dependent and is proportional to the ribosome concentrations. Scatchard analysis of the binding data reveals that the dissociation constant (Kd) is about 20 microM. The binding of eperezolid to the ribosome is competitively inhibited by chloramphenicol and lincomycin. However, unlike chloramphenicol and lincomycin, eperezolid does not inhibit the puromycin reaction, indicating that the oxazolidinones have no effect on peptidyl transferase [2]. eperezolid was found to bind only to the 50S subunit, with similar affinity as to the 70S ribosome, and to have no affinity for the 30S subunit [3].
Erythromycin, an oral macrolide antibiotic produced by Streptomyces erythreus, reversibly binds to the 50S ribosome of bacteria, and inhibits protein synthesis.
Target: Antibacterial
Erythromycin is a macrolide antibiotic that has an antimicrobial spectrum similar to or slightly wider than that of penicillin, and is often prescribed for people who have an allergy to penicillins. For respiratory tract infections, it has better coverage of atypical organisms, including Mycoplasma and legionellosis. It was first marketed by Eli Lilly and Company, and it is today commonly known as EES (erythromycin ethylsuccinate, an ester prodrug that is commonly administered). It is also occasionally used as a prokinetic agent.
Erythromycin estolate has been associated with reversible hepatotoxicity in pregnant women in the form of elevated serum glutamic-oxaloacetic transaminase and is not recommended during pregnancy. Some evidence suggests similar hepatotoxicity in other populations. Erythromycin displays bacteriostatic activity or inhibits growth of bacteria, especially at higher concentrations, but the mechanism is not fully understood. By binding to the 50s subunit of the bacterial 70s rRNA complex, protein synthesis and subsequent structure and function processes critical for life or replication are inhibited. Erythromycin interferes with aminoacyl translocation, preventing the transfer of the tRNA bound at the A site of the rRNA complex to the P site of the rRNA complex. Without this translocation, the A site remains occupied and, thus, the addition of an incoming tRNA and its attached amino acid to the nascent polypeptide chain is inhibited. This interferes with the production of functionally useful proteins, which is the basis of this antimicrobial action.
Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.
Target: Antibacterial
Ethambutol directly affects two polymers, arabinogalactan (AG) and lipoarabinomannan (LAM) in Mycobacterium smegmatis. In M. smegmatis, Ethambutol inhibits synthesis of arabinan completely and inhibits AG synthesis most likely as a consequence of this; more than 50% of the cell arabinan is released from the bacteria following Ethambutol treatment, whereas no galactan is released. Ethambutol main targets against embB gene product in M. avium. Ethambutol induces 60% changes in the embB gene in M. tuberculosis resistant mutants [1]. Ethambutol is effective against actively growing microorganisms of the genus Mycobacterium, including M. tuberculosis. Nearly all strains of M. tuberculosis and M. kansasii as well as a number of strains of the M. aviumcomplex (MAC) are sensitive to Ethambutol. [1] Ethambutol is potency against M. tuberculosis (H37Rv) with MIC of 0.5 μg/mL in vitro [2]. Ethambutol is efficient on treatment of mycobacterial-infected macrophages. When M. tuberculosis infected macrophages are treated with 6 μg/mL Ethambutol, the log CFUs following treatment for 3 days is 4.17, while value in control group is 4.8. The MICs for M. avium (MTCC 1723) and M. smegmatis (MTCC 6) are 15 μg/mL and 0.18 μg/mL, respectively. Ethambutol is efficient in animal model. 100 mg/kg Ethambutol given orally 15 days post i.v. infection 1 ×/week for 5 weeks, induces a lower log CFU compared with untreatment (4.59 vs 5.07) [3].
Ethambutol Dihydrochloride is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.
Target: Antibacterial
Ethambutol directly affects two polymers, arabinogalactan (AG) and lipoarabinomannan (LAM) in Mycobacterium smegmatis. In M. smegmatis, Ethambutol inhibits synthesis of arabinan completely and inhibits AG synthesis most likely as a consequence of this; more than 50% of the cell arabinan is released from the bacteria following Ethambutol treatment, whereas no galactan is released. Ethambutol main targets against embB gene product in M. avium. Ethambutol induces 60% changes in the embB gene in M. tuberculosis resistant mutants [1]. Ethambutol is effective against actively growing microorganisms of the genus Mycobacterium, including M. tuberculosis. Nearly all strains of M. tuberculosis and M. kansasii as well as a number of strains of the M. aviumcomplex (MAC) are sensitive to Ethambutol. [1] Ethambutol is potency against M. tuberculosis (H37Rv) with MIC of 0.5 μg/mL in vitro [2]. Ethambutol is efficient on treatment of mycobacterial-infected macrophages. When M. tuberculosis infected macrophages are treated with 6 μg/mL Ethambutol, the log CFUs following treatment for 3 days is 4.17, while value in control group is 4.8. The MICs for M. avium (MTCC 1723) and M. smegmatis (MTCC 6) are 15 μg/mL and 0.18 μg/mL, respectively. Ethambutol is efficient in animal model. 100 mg/kg Ethambutol given orally 15 days post i.v. infection 1 ×/week for 5 weeks, induces a lower log CFU compared with untreatment (4.59 vs 5.07) [3].
Ethionamide(2-ethylthioisonicotinamide) is an antibiotic used in the treatment of tuberculosis.
Target: Antibacterial
Ethionamide is a second-line antitubercular agent that inhibits mycolic acid synthesis. It also may be used for treatment of leprosy. Ethionamide is a prodrug. It is activated by the enzyme EthA, a mono-oxygenase in Mycobacterium tuberculosis, and binds NAD+ to form an adduct which inhibits InhA in the same way as isoniazid. Expression of the ethA gene is controlled by EthR, a transcriptional repressor. It is understood that improving ethA expression will increase the efficacy of ethionamide and so EthR inhibitors are of great interest to co-drug developers. The action may be through disruption of mycolic acid [1, 2].
Faropenem daloxate is the first oral penem in a new class of beta-lactam antibiotics.
IC50 Value:
Target: Antibacterial
Faropenem daloxate is useful for penem and antibiotics. Faropenem medoxomil has excellent in vitro activity against Streptococcus pneumoniae, Haemophilus influenzae and other key pathogens implicated in acute bacterial rhinosinusitis. Clinical studies have demonstrated that, in the treatment of acute bacterial rhinosinusitis in adults, 7 days of treatment with faropenem medoxomil is as clinically and bacteriologically effective as 10 days of treatment with cefuroxime axetil. One study showed faropenem medoxomil to be superior to cefuroxime axetil. Overall, the safety profile of faropenem medoxomil is similar to that of most comparators.
Fidaxomicin(OPT-80; PAR-101) is a new class of narrow spectrum macrocyclic antibiotic drug; selective eradication of pathogenic Clostridium difficile with minimal disruption to the multiple species of bacteria that make up the normal, healthy intestinal flora.
Fleroxacin is a broad-spectrum antimicrobial fluoroquinolone.
Target: Antibacterial
Fleroxacin (Ro 23-6240; AM-833) is a new trifluorinated quinolone exhibiting high activity against a broad spectrum of gram-negative and gram-positive bacteria. Fleroxacin is characterized pharmacokinetically by a long elimination half-life (9 to 10 h) and high concentrations in plasma (e.g., maximum concentration of 2.3 micrograms/ml after an oral dose of 200 mg) [1]. Fleroxacin is effective against Haemophilus ducreyi in vitro. Fleroxacin, 200 or 400 mg as a single oral dose, is efficacious therapy for microbiologically proven chancroid in patients who do not have concurrent HIV-1 infection. Among HIV-1-infected men, a single dose of 200 or 400 mg of fleroxacin is inadequate therapy for chancroid [2, 3].
Flumequine is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM.
Target: Topoisomerase II; Antibacterial
Flumequine has minimum inhibitory concentration (MIC) ranging from 0.06 μg/mL to 32 μg/mL in 12 clinical A. salmonicida isolates. Flumequine enhibits high E(max) values of 16 for the most resistant isolates, which indicates an important contribution of efflux to the resistance phenotype. Flumequine accumulation experiments confirmes that high E(max) values are associated with a much lower level of accumulation [1].
Flumequine shows the bioavailability of 44.7% following oral administration of medicated feed in Atlantic salmon. Flumequine results in the volumes of distribution at steady state of 3.5 L/kg, elimination half-life (t 1/2) of 22.8 hours and area under plasma drug concentration-time curve (AUC) of 140 μg×hours/mL following intravenous administration in Atlantic salmon [2].
Flumequine (10 mg/kg, oral) results in the volumes of distribution at steady-state (Vss) of 2.41 L/kg (cod) and 2.15 L/kg (wrasse) following intravenous administration. Total body clearances (Cl) are 0.024 L/h.kg (cod) and 0.14 L/h.kg (wrasse) and the elimination half-lives (t1/2 λ z) are calculated to be 75 hours (cod) and 31 hours (wrasse) after Flumequine (10 mg/kg, oral) administration. The oral bioavailabilities (F) are calculated to be 65% (cod) and 41% (wrasse) following oral administration of Flumequine [3].
Furagin, nitrofurantoin analog, is an anti-bacterial agent. Furagin is 2-substituted 5-nitrofuran, chemically and structurally similar to well-known antibacterial compound nitrofurantoin.
IC50 Value:
Target: Antibacterial
in vitro: The furagin concentrations in serum remain several hours above the MIC concentrations of many pathogenic bacteria. Despite the high concentrations in serum, the urine levels of furagin were generally lower than those of nitrofurantoin. The 24 hr recoveries in urine were 8--13% for furagin and about 36% for nitrofurantoin [1].
in vivo: A time-independent increase in SCE frequency was found in lymphocytes of children treated with furagin. Total CA frequency did not differ significantly between groups of children with various duration of furagin treatment [2]. Women were randomised into two groups receiving either ciprofloxacin 250mg twice a day for 3 days (n=13) or furagin 100mg three times a day for 7 days (n=14). Median lengths of follow-up were 4 days and 5 days in the ciprofloxacin and furagin groups, respectively [3].
Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, it inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.
Target: Antibacterial
Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. Gatifloxacin had activity equal to that of tosufloxacin and activity more potent than those of norfloxacin, ofloxacin, ciprofloxacin, and sparfloxacin against the second-step mutants (grlA gyrA; gatifloxacin MIC range, 1.56 to 3.13 microg/ml) and had the most potent activity against the third-step mutants (grlA gyrA grlA; gatifloxacin MIC range, 1.56 to 6.25 microg/ml), suggesting that gatifloxacin possesses the most potent inhibitory activity against singly mutated topo IV and singly mutated DNA gyrase among the quinolones tested [1].
Ophthalmic gatifloxacin 0.3% is at least as effective as ciprofloxacin at healing corneal ulcers infected with Pseudomonas aeruginosa when gatifloxacin is administered less frequently than ciprofloxacin. Trends favored gatifloxacin in fluorescein retention scores [2].
Clinical indications: Bacterial infection
FDA Approved Date:
Toxicity: Hepatotoxicity; Acute pancreatitis [3]; Torsades de pointes [4]
Gatifloxacin (hydrochloride) is an antibiotic of the fourth-generation fluoroquinolone family, it inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.
Target: Antibacterial
Gatifloxacin (hydrochloride) is the hydrochloride salt of Gatifloxacin which is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. Gatifloxacin had activity equal to that of tosufloxacin and activity more potent than those of norfloxacin, ofloxacin, ciprofloxacin, and sparfloxacin against the second-step mutants (grlA gyrA; gatifloxacin MIC range, 1.56 to 3.13 microg/ml) and had the most potent activity against the third-step mutants (grlA gyrA grlA; gatifloxacin MIC range, 1.56 to 6.25 microg/ml), suggesting that gatifloxacin possesses the most potent inhibitory activity against singly mutated topo IV and singly mutated DNA gyrase among the quinolones tested [1].
Ophthalmic gatifloxacin 0.3% is at least as effective as ciprofloxacin at healing corneal ulcers infected with Pseudomonas aeruginosa when gatifloxacin is administered less frequently than ciprofloxacin. Trends favored gatifloxacin in fluorescein retention scores [2].
Clinical indications: Bacterial infection
FDA Approved Date:
Toxicity: Hepatotoxicity; Acute pancreatitis [3]; Torsades de pointes [4]
Gatifloxacin (mesylate) is an antibiotic of the fourth-generation fluoroquinolone family, it inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.
Target: Antibacterial
Gatifloxacin (mesylate) is the mesylate salt of Gatifloxacin which is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. Gatifloxacin had activity equal to that of tosufloxacin and activity more potent than those of norfloxacin, ofloxacin, ciprofloxacin, and sparfloxacin against the second-step mutants (grlA gyrA; gatifloxacin MIC range, 1.56 to 3.13 microg/ml) and had the most potent activity against the third-step mutants (grlA gyrA grlA; gatifloxacin MIC range, 1.56 to 6.25 microg/ml), suggesting that gatifloxacin possesses the most potent inhibitory activity against singly mutated topo IV and singly mutated DNA gyrase among the quinolones tested [1].
Ophthalmic gatifloxacin 0.3% is at least as effective as ciprofloxacin at healing corneal ulcers infected with Pseudomonas aeruginosa when gatifloxacin is administered less frequently than ciprofloxacin. Trends favored gatifloxacin in fluorescein retention scores [2].
Clinical indications: Bacterial infection
Toxicity: Hepatotoxicity; Acute pancreatitis [3]; Torsades de pointes [4]
Hexamethylenetetramine(Methenamine) is an antibiotic used for the treatment of urinary tract infection.
Target: Antibacterial
Using an in vitro system that simulates the dynamics of the urinary tract, it is shown that concentrations of formaldehyde > 25 μg/ml can be achieved in urine containing > 0.6 mg of methenamine per ml at pH < 5.7 or > 1 mg/ml at pH < 5.85. Exposure to this concentration of formaldehyde for 2 h produces a measurable antibacterial effect [1, 2].
Hygromycin B, a selective antibiotic that is effective on most bacteria, fungi and higher eukaryotes.
Target: Antifungal; Antibacterial
Hygromycin B is an antibiotic produced by the bacterium Streptomyces hygroscopicus. It is an aminoglycoside that kills bacteria, fungi and higher eukaryotic cells by inhibiting protein synthesis. Hygromycin B has a single binding site within the 30S, it locates in the major groove of the helix very close to the helical axis, and makes contact with nucleotides from both RNA strands in the region 1490-1500 and 1400-1410. Ring I of HygB is involved in nonsequence-specific interactions with the backbone phosphate oxygen atoms of G1494 in addition to base-specific interactions with G1494 and U1495. Rings II and III make weak base-specific hydrogen bonds to both C1404 and U1498, but their main role apparently is to position ring IV for interaction with bases in the 1496-1498 region. Ring IV of HygB comes within 4A of the second base of the P site bound mRNA codon [1]. Hygromycin B (0.38 mM) completely halts yeast cell growth in rich media. Hygromycin B strongly block Polypeptide synthesis in cell-free extracts from rabbit reticulocytes, wheat germ and yeast. Hygromycin B inhibits peptide chain elongation by yeast polysomes by preventing elongation factor EF-2-dependent translocation [2]. Hygromycin B inhibits (80%) the elogation-factor-(EF)G-plus-GTP-dependent reaction of either AcPhe-tRNA or natural peptideyl-tRNA with puromycin in Escherichia coli cell-free systems. Hygromycin B blocks the nascnet peptide chains of either purified endogenous E. coli polysomes or poly(uridylic acid)-programmed ribosomes during polypeptide synthesis. Hygromycin B inhibits the non-enzymic translocation and the release of AcPhe-tRNA from the ribosomal acceptor site promoted by depletion of NH4 ions [3].
I2906 showed antimycobacterial and cytotoxic activity against mycobacterium tuberculosis.
IC50 Value:
Target: Antibacterial
Under in vitro conditions, I2906 showed excellent antimycobacterial activities and low cytotoxicity. In a murine model infected with M. tuberculosis H37Rv, the reductions on bacterial loads of both lungs and spleen were statistically significant (p < 0.05) between I2906-treated mice and untreated controls after 4 weeks. Further, the colony-forming unit counts in the lungs were dramatically lower (p < 0.05) than that of isoniazid-treated mice by the addition of I2906 after 8 weeks. Moreover, survival rate was increased by I2906 treatment. For multidrug-resistant strain infection, bacterial counts were reduced significantly in the lungs and spleen due to I2906 treatment in comparison with data from untreated controls (p < 0.05).
Isoniazid is an antibacterial agent used primarily as a tuberculostatic.
Target: Antibacterial
Isoniazid is a prodrug and must be activated by a bacterial catalase-peroxidase enzyme that in M. tuberculosis is called KatG [1]. KatG couples the isonicotinic acyl with NADH to form isonicotinic acyl-NADH complex. This complex binds tightly to the enoyl-acyl carrier protein reductase known as InhA, thereby blocking the natural enoyl-AcpM substrate and the action of fatty acid synthase. This process inhibits the synthesis of mycolic acid, required for the mycobacterial cell wall. A range of radicals are produced by KatG activation of isoniazid, including nitric oxide, which has also been shown to be important in the action of another antimycobacterial prodrug PA-824 [2, 3]. Isoniazid is bactericidal to rapidly dividing mycobacteria, but is bacteriostatic if the mycobacteria are slow-growing [4].
Kanamycin sulfate is an aminoglycoside bacteriocidal antibiotic.
IC50 Value:
Target: Antibacterial
Kanamycin (also known as kanamycin A) is an aminoglycoside antibiotic effective against Gram-positive and Gram-negative organisms. Inhibitor of protein biosynthesis that acts on the 30S ribosome, causing misreading of the genetic code. Kanamycin may cause renal damage and ototoxicity.
Levofloxacin, a synthetic fluoroquinolone, is an antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.
Target: Antibacterial
Levofloxacin reduced bacterial load compared with placebo by 4.9-fold (95% confidence interval, 1.4-25.7; P=0.02) at day 7 but had no effect at any point on any marker of neutrophilic airway inflammation. In patients with a baseline bacterial load of more than 10(6) cfu/mL, levofloxacin treatment was associated with a 26.5% (95% confidence interval, 1.8%-51.3%; P=0.04) greater reduction in the percentage neutrophil count compared with placebo at day 7 [1]. Levofloxacin was found to significantly improve the clinical and microbiological parameters in CP individuals [2]. A 30-day course of levofloxacin does not significantly improve BK viral load reduction or allograft function when used in addition to overall reduction of immunosuppression [3].
Lincomycin Hydrochloride(U10149A) is an antibiotic produced by Streptomyces lincolnensis var. lincolnensis.
Target: Antibacterial
Lincomycin hydrochloride is a systemic antibiotic, which is active against most common gram positive bacteria. It has proved to be excellent for infectious diseases like acne, anthrax, pneumonia, and also for the treatment of furunculosis, carbuncles, impetigo, burns and wounds, carrying to gram positive bacteria. Lincomycin hydrochloride inhibits cell growth and microbial protein synthesis, by interacting strongly and specifically with the 50S ribosomal subunit, at mutually related sites [1-3].
Linezolid(Zyvoxid) is a synthetic antibiotic used for the treatment of serious infections caused by Gram-positive bacteria that are resistant to several other antibiotics.
IC50 value:
Target: Antibiotic
A member of the oxazolidinone class of drugs, linezolid is active against most Gram-positive bacteria that cause disease, including streptococci, vancomycin-resistant enterococci (VRE), and methicillin-resistant Staphylococcus aureus (MRSA).
Lomefloxacin(SC47111A) is a fluoroquinolone antibiotic.
Target: Antibacterial
Lomefloxacin is a bactericidal fluoroquinolone agent with activity against a wide range of gram-negative and gram-positive organisms. The bactericidal action of lomefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited [1].
Lomefloxacin HCl is a fluoroquinolone antibiotic.
Target: Antibacterial
Lomefloxacin is a bactericidal fluoroquinolone agent with activity against a wide range of gram-negative and gram-positive organisms. The bactericidal action of lomefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited [1].
MAC13243, an antibacterial agent, is a likely inhibitor of the bacterial lipoprotein targeting chaperone, LolA.
IC50 Value:
Target: Antibacterial
MAC13243, a molecule that belongs to a new chemical class and that has a unique mechanism and promising activity against multidrug-resistant Pseudomonas aeruginosa. MAC13243 inhibits the function of the LolA protein and represents a new chemical probe of lipoprotein targeting in bacteria with promise as an antibacterial lead with Gram-negative selectivity.
Mafenide is a sulfonamide-type medication.
Target: Antibacterial
Mafenide is a sulfonamide-type medication. Mafenide works by reducing the bacterial population present in the avascular tissues of burns and permits spontaneous healing of deep partial-thickness burns. It is used to treat severe burns. It is used topically as an adjunctive therapy for second- and third-degree burns. It is bacteriostatic against many gram-positive and gram-negative organisms, including Pseudomonas aeruginosa. Some sources state that mafenide is more appropriate for non-facial burns, while chloramphenicol/prednisolone or bacitracin are more appropriate for facial burns [1-3].
Mafenide Acetate is a sulfonamide-type medication.
Target: Others
Mafenide is a sulfonamide-type medication. Mafenide works by reducing the bacterial population present in the avascular tissues of burns and permits spontaneous healing of deep partial-thickness burns. It is used to treat severe burns. It is used topically as an adjunctive therapy for second- and third-degree burns. It is bacteriostatic against many gram-positive and gram-negative organisms, including Pseudomonas aeruginosa. Some sources state that mafenide is more appropriate for non-facial burns, while chloramphenicol/prednisolone or bacitracin are more appropriate for facial burns [1-3].
Marbofloxacin is a potent antibiotic of which depends upon its inhibition of DNA-gyrase. Marbofloxacin is a synthetic, broad spectrum bactericidal agent.
Target: DNA-gyrase
Marbofloxacin is a third-generation fluoroquinolone for veterinary use, the antimicrobial of which depends upon its inhibition of DNA-gyrase and topoisomerase IV. With a broad spectrum bactericidal activity and good efficacy, marbofloxacin is indicated for dermatological, respiratory and urinary tract infections due to both Gram-positive and Gram-negative bacteria and Mycoplasma [1].
Administration of Marbofloxacin at 6 mg/kg once daily for 7 days in a Staphylococcus aureus infection in tissue cages in ponies is not effective for the elimination of S. aureus infections from secluded sites [2]. The pharmacokinetic properties of marbofloxacin were investigated in 6 horses after i.v., subcutaneous and oral administration of a single dose of 2 mg/kg bwt and the minimal inhibitory concentrations (MIC) assessed for bacteria isolated from equine infectious pathologies. The clearance of marbofloxacin was mean +/- s.d. 0.25 +/- 0.05 l/kg/h and the terminal half-life 756 +/- 1.99 h. The marbofloxacin absolute bioavailabilities after subcutaneous and oral administration were 98 +/- 11% and 62 +/- 8%, respectively. Considering the breakpoint values of efficacy indices for fluoroquinolones, a marbofloxacin dosage regimen of 2 mg/kg bwt/24 h by i.v., subcutaneous or oral routes was more appropriate for enterobacteriaceae than for S. aureus [3].
Toxicity: cramps; vomiting; anorexia; soft stools; diarrhoea
Marbofloxacin hydrochloride is a potent antibiotic of which depends upon its inhibition of DNA-gyrase.
Target: DNA-gyrase
Marbofloxacin hydrochloride is a third-generation fluoroquinolone for veterinary use, the antimicrobial of which depends upon its inhibition of DNA-gyrase and topoisomerase IV. With a broad spectrum bactericidal activity and good efficacy, marbofloxacin hydrochloride is indicated for dermatological, respiratory and urinary tract infections due to both Gram-positive and Gram-negative bacteria and Mycoplasma [1].
Administration of Marbofloxacin hydrochloride at 6 mg/kg once daily for 7 days in a Staphylococcus aureus infection in tissue cages in ponies is not effective for the elimination of S. aureus infections from secluded sites [2]. The pharmacokinetic properties of marbofloxacin hydrochloride were investigated in 6 horses after i.v., subcutaneous and oral administration of a single dose of 2 mg/kg bwt and the minimal inhibitory concentrations (MIC) assessed for bacteria isolated from equine infectious pathologies. The clearance of marbofloxacin hydrochloride was mean +/- s.d. 0.25 +/- 0.05 l/kg/h and the terminal half-life 756 +/- 1.99 h. The marbofloxacin hydrochloride absolute bioavailabilities after subcutaneous and oral administration were 98 +/- 11% and 62 +/- 8%, respectively. Considering the breakpoint values of efficacy indices for fluoroquinolones, a marbofloxacin hydrochloride dosage regimen of 2 mg/kg bwt/24 h by i.v., subcutaneous or oral routes was more appropriate for enterobacteriaceae than for S. aureus [3].
Toxicity: cramps; vomiting; anorexia; soft stools; diarrhoea
Meropenem is a carbapenem antibiotic, which displaying a broad spectrum of antibacterial activity.
Target: Antibacterial
Meropenem, a new parenteral carbapenem demonstrated increased activity as compared to imipenem against 336 strains of Neisseria gonorrhoeae, 119 strains of Haemophilus influenzae, and 110 strains of H. Ceftriaxone and ciprofloxacin demonstrated activity superior to that of both carbapenems while the activity of ceftazidime was similar to that of meropenem [1]. Meropenem, like imipenem and various experimental penems, may overcome the resistance problems presented by Class I beta-lactamases [2]. MEROPENEM was rapidly penetrated to the pleural effusion and was retained for a more prolonged time in the pleural effusion than in the blood of patients with accumulated pleural effusion, and it suggested the usefulness of MEROPENEM in antibacterial therapy for patients with pleurisy causing accumulation of pleural effusion [3].
Clinical indications: Appendicitis; Bacterial infection; Bacterial meningitis; Bacterial pneumonia; Bacterial respiratory tract infection; Bacterial skin infection; Bacterial urinary tract infection; Bacteroides fragilis infection; Bacteroides infection; Bacteroides thetaiotaomicron infection; Complicated skin and skin structure infection
FDA Approved Date: July 1996
Toxicity: In mice and rats, large intravenous doses of meropenem (2200-4000 mg/kg) have been associated with ataxia, dyspnea, convulsions, and mortalities.
Meropenem (trihydrate) is a carbapenem antibiotic, which displaying a broad spectrum of antibacterial activity.
Target: Antibacterial
Meropenem (trihydrate), a new parenteral carbapenem demonstrated increased activity as compared to imipenem against 336 strains of Neisseria gonorrhoeae, 119 strains of Haemophilus influenzae, and 110 strains of H. Ceftriaxone and ciprofloxacin demonstrated activity superior to that of both carbapenems while the activity of ceftazidime was similar to that of meropenem [1]. Meropenem (trihydrate), like imipenem and various experimental penems, may overcome the resistance problems presented by Class I beta-lactamases [2]. Meropenem (trihydrate) was rapidly penetrated to the pleural effusion and was retained for a more prolonged time in the pleural effusion than in the blood of patients with accumulated pleural effusion, and it suggested the usefulness of Meropenem (trihydrate) in antibacterial therapy for patients with pleurisy causing accumulation of pleural effusion [3].
Clinical indications: Appendicitis; Bacterial infection; Bacterial meningitis; Bacterial pneumonia; Bacterial respiratory tract infection; Bacterial skin infection; Bacterial urinary tract infection; Bacteroides fragilis infection; Bacteroides infection; Bacteroides thetaiotaomicron infection; Complicated skin and skin structure infection
FDA Approved Date: July 1996
Toxicity: In mice and rats, large intravenous doses of meropenem (2200-4000 mg/kg) have been associated with ataxia, dyspnea, convulsions, and mortalities.
Methacycline HCl is a tetracycline antibiotic.
Target: Antibacterial
Methacycline HCl is a broad-spectrum semisynthetic antibiotic related to tetracycline but excreted more slowly and maintaining effective blood levels for a more extended period.
Metronidazole is a nitroimidazole antibiotic medication used particularly for anaerobic bacteria and protozoa.
Target: Antibacterial; Antiparasitic
Metronidazole is a nitroimidazole antibiotic medication used particularly for anaerobic bacteria and protozoa. Metronidazole is an antibiotic, amebicide, and antiprotozoal.[1] It is the drug of choice for first episodes of mild-to-moderate Clostridium difficile infection [2]. Metronidazole, taken up by diffusion, is selectively absorbed by anaerobic bacteria and sensitive protozoa. Once taken up by anaerobes, it is non-enzymatically reduced by reacting with reduced ferredoxin, which is generated by pyruvate oxido-reductase. Many of the reduced nitroso intermediates will form sulfinamides and thioether linkages with cysteine-bearing enzymes, thereby deactivating these critical enzymes. As many as 150 separate enzymes are affected.In addition or alternatively, the metronidazole metabolites are taken up into bacterial DNA, and form unstable molecules. This function only occurs when metronidazole is partially reduced, and because this reduction usually happens only in anaerobic cells, it has relatively little effect upon human cells or aerobic bacteria.[3]
Minocycline is a tetracycline antibiotic with neuroprotective, antiapoptotic, anti-inflammatory and antimicrobial effects.
IC50 Value: N/A
Target: Antibacterial
Minocycline acts as a matrix metalloproteinase (MMP) inhibitor; attenuates disease severity in mouse models of multiple sclerosis. Minocycline also inhibit the enzymatic activity of poly(ADP-ribose) polymerase-1 (PARP-1) and angiogenesis. In addition, Minocycline is suggested to down-regulate CD40L on T cells and inhibit the replication of SIV and HIV. Orally active and brain penetrant.
Moxifloxacin is a synthetic fluoroquinolone antibiotic agent.
Target: Antibacterial
Moxifloxacin is an extended-spectrum fluoroquinolone which has improved coverage against gram-positive cocci and atypical pathogens compared with older fluoroquinolone agents, while retaining good activity against gram-negative bacteria. The antibacterial spectrum of moxifloxacin includes all major upper and lower respiratory tract pathogens; it is one of the most active fluoroquinolones against pneumococci, including penicillin- and macrolide-resistant strains [1]. Moxifloxacin has limited phototoxic potential. In clinical trials, moxifloxacin had clinical success rates of 88-97% and bacteriologic eradication rates of 90-97%. Moxifloxacin is a safe and effective antimicrobial that will be useful for treating acute sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia [2]. Moxifloxacin possibly stimulates lipid peroxidation and enhances phagocytosis, as depicted by MDA production and survival prolongation, without being toxic as depicted by white blood cell count [3].
Clinical indications: Abdominal abscess; Acute bronchitis; Acute sinusitis; Bacterial infection
Toxicity: Symptoms of overdose include CNS and gastrointestinal effects such as decreased activity, somnolence, tremor, convulsions, vomiting, and diarrhea. The minimal lethal intravenous dose in mice and rats is 100 mg/kg.
Moxifloxacin (Hydrochloride) is a synthetic fluoroquinolone antibiotic agent.
Target: Antibacterial
Moxifloxacin is an extended-spectrum fluoroquinolone which has improved coverage against gram-positive cocci and atypical pathogens compared with older fluoroquinolone agents, while retaining good activity against gram-negative bacteria. The antibacterial spectrum of moxifloxacin includes all major upper and lower respiratory tract pathogens; it is one of the most active fluoroquinolones against pneumococci, including penicillin- and macrolide-resistant strains [1]. Moxifloxacin has limited phototoxic potential. In clinical trials, moxifloxacin had clinical success rates of 88-97% and bacteriologic eradication rates of 90-97%. Moxifloxacin is a safe and effective antimicrobial that will be useful for treating acute sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia [2]. Moxifloxacin possibly stimulates lipid peroxidation and enhances phagocytosis, as depicted by MDA production and survival prolongation, without being toxic as depicted by white blood cell count [3].
Clinical indications: Abdominal abscess; Acute bronchitis; Acute sinusitis; Bacterial infection
Toxicity: Symptoms of overdose include CNS and gastrointestinal effects such as decreased activity, somnolence, tremor, convulsions, vomiting, and diarrhea. The minimal lethal intravenous dose in mice and rats is 100 mg/kg.
Nadifloxacin(OPC7251) is a topical fluoroquinolone antibiotic for the treatment of acne vulgaris.
Target: Antibacterial
Nadifloxacin is a potent, broad-spectrum, quinolone agent approved for topical use in acne vulgaris and skin infections. Nadifloxacin inhibits the enzyme DNA gyrase that is involved in bacterial DNA synthesis and replication, thus inhibiting the bacterial multiplication. In vitro studies of nadifloxacin show potent and broad-spectrum antibacterial activity against aerobic Gram-positive, Gram-negative and anaerobic bacteria. Additionally, studies also suggest that the effectiveness of nadifloxacin in inflammatory acne lesions may be attributed to its inhibitory effect on pro-inflammatory cytokines like interleukin (IL)-1α, IL-6, and IL-8 which also play an important role in acne pathogenesis [1, 2].
Nafcillin sodium monohydrate is a semi-synthetic antibiotic related to penicillin.
Target: Antibacterial
Nafcillin sodium is a narrow-spectrum, beta-lactam antibiotic of the penicillin class. As a beta-lactamase-resistant penicillin, it is used to treat infections caused by Gram-positive bacteria, in particular, species of staphylococci that are resistant to other penicillins. Nafcillin is considered therapeutically equivalent to oxacillin, although its safety profile is somewhat different. Nafcillin was shown to reversibly inhibit beta-lactamase from Staphylococcus aureus PC1 with characteristics indicative of a type A inhibitor [Citri, Samuni & Zyk (1976) Proc. Natl. Acad. Sci. U.S.A. 73, 1048-1052]. At nafcillin concentrations above 80 mM, complete inactivation occurred within 200 s. Upon removal of the excess nafcillin the inhibited enzyme was re-activated completely, with a rate constant of 2.0 x 10(-3) s-1 (25 degrees C) [1, 2].
Nalidixic acid is a synthetic 1,8-naphthyridine antimicrobial agent with a limited bacteriocidal spectrum.
Target: Antibacterial
Nalidixic acid is the first of the synthetic quinolone antibiotics. Nalidixic acid is effective against both gram-positive and gram-negative bacteria. In lower concentrations, it acts in a bacteriostatic manner; that is, it inhibits growth and reproduction. In higher concentrations, it is bactericidal, meaning that it kills bacteria instead of merely inhibiting their growth. Nalidixic selectively and reversibly blocks DNA replication in susceptible bacteria. Nalidixic acid and related antibiotics inhibit a subunit of DNA gyrase and topoisomerase IV and induce formation of cleavage complexes. It also inhibits the nicking-closing activity on the subunit of DNA gyrase that releases the positive binding stress on the supercoiled DNA. From Wikipedia.
Neomycin Sulfate is an aminoglycoside antibiotic and calcium channel protein inhibitor.
Target: Calcium Channel; Antibacterial
Neomycin inhibits thrombin-stimulated release of inositol 1,4,5-trisphosphate (IP3), by selectively binding PIP2, but does not inhibit 32P incorporation into PI or initiation of DNA synthesis [1]. Neomycin (10 microM - 1 mM) was found to induce considerable release of [3H]arachidonic acid from phosphatidylinositol, phosphatidylcholine and phosphatidylethanolamine in saponin-permeabilized human platelets prelabeled with [3H]arachidonic acid. neomycin enhanced arachidonic acid release induced by thrombin [2, 3]. Neomycin similarly inhibited PLD activity present in rat brain membranes and assayed in vitro with [3H]phosphatidylcholine as substrate (50% inhibition at 65 microM) [4].
Nifuratel(NF 113, SAP 113) is a broad antibacterial spectrum agent, which is used as an antibacterial, antifungal, and antiprotozoal (Trichomonas).
IC50 Value: 0.125-1 μg/mL(MIC, A. vaginae) [1]
Target: Antibacterial; Antiprotozoal
in vitro: In vitro, nifuratel is able to inhibit the growth of A. vaginae, with a MIC range of 0.125-1 μg/mL; it is active against G. vaginalis and does not affect lactobacilli [1].
in vivo: Patients were randomized to receive a 2-week course of bismuth subcitrate (8 mg/kg/day, q.d.s.), amoxicillin (50 mg/kg/day, q.d.s.), with either nifuratel (15 mg/kg/day, q.d.s.) or furazolidone (10 mg/kg/day, q.d.s.), plus omeprazole (0.5 mg/kg, once daily) [2].
Toxicity: There were no serious adverse reactions and were no withdrawals due to any side-effects. All of side-effects were self-limiting (dark stools, urine discoloration, blackening of the tongue, and others) [3].
Clinical trial: N/A
Nitrofural is a bactericidal compound used as an antibiotic most commonly in the form of ointments.
Target: Antibacterial
Nitrofurazone, a nitroaromatic drug, is a broad spectrum antibiotic which has until now been considered as activated in bacteria by nitroreductases. Its use in medicine has become less frequent as safer and more effective products have become available, and it has been discontinued in the US.
Nitrofurazone (NF) and its derivative, hydroxymethylnitrofurazone (NFOH), have presented antichagasic activity. In vitro cruzain inhibition tests were performed for both compounds, and the 50% inhibitory concentration (IC50) for NF and NFOH presented values of 22.83 ± 1.2 μM and 10.55 ± 0.81 μM, respectively. AM1 semi-empirical molecular modeling studies were performed to understand the activity of the compounds, corroborating the observed cruzain inhibitory activity.
Norfloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria, which functions by inhibiting DNA gyrase.
Target: DNA gyrase; Antibacterial
Norfloxacin is a synthetic chemotherapeutic antibacterial agent occasionally used to treat common as well as complicated urinary tract infections. Norfloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. It functions by inhibiting DNA gyrase, a type II topoisomerase, and topoisomerase IV, enzymes necessary to separate bacterial DNA, thereby inhibiting cell division.There are currently three approved uses in the adult population (one of which is restricted) and the other ineffective due to bacterial resistance. Chibroxin (ophthalmic) is approved for use in children older than one year of age.
Norfloxacin is associated with a number of rare serious adverse reactions as well as spontaneous tendon ruptures and irreversible peripheral neuropathy. Tendon problems may manifest long after therapy had been completed and in severe cases may result in lifelong disabilities. Hepatoxicity resulting in fatalities has also been reported with the use of norfloxacin.
Norfloxacin hydrochloride is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria, which functions by inhibiting DNA gyrase.
Target: DNA gyrase; Antibacterial
Norfloxacin is a synthetic chemotherapeutic antibacterial agent occasionally used to treat common as well as complicated urinary tract infections. Norfloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. It functions by inhibiting DNA gyrase, a type II topoisomerase, and topoisomerase IV, enzymes necessary to separate bacterial DNA, thereby inhibiting cell division.There are currently three approved uses in the adult population (one of which is restricted) and the other ineffective due to bacterial resistance. Chibroxin (ophthalmic) is approved for use in children older than one year of age.
Norfloxacin is associated with a number of rare serious adverse reactions as well as spontaneous tendon ruptures and irreversible peripheral neuropathy. Tendon problems may manifest long after therapy had been completed and in severe cases may result in lifelong disabilities. Hepatoxicity resulting in fatalities has also been reported with the use of norfloxacin.
Novobiocin Sodium is an antibiotic compound derived from Streptomyces niveus.
Target: Antibacterial
Novobiocin, also known as albamycin or cathomycin, is an aminocoumarin antibiotic that is produced by the actinomycete Streptomyces niveus, which has recently been identified as a subjective synonym for S. spheroides a member of the order Actinobacteria . Other aminocoumarin antibiotics include clorobiocin and coumermycin A1. The molecular basis of action of novobiocin, and other related drugs clorobiocin and coumermycin A1 has been examined. Aminocoumarins are very potent inhibitors of bacterial DNA gyrase and work by targeting the GyrB subunit of the enzyme involved in energy transduction. Novobiocin as well as the other aminocoumarin antibiotics act as competitive inhibitors of the ATPase reaction catalysed by GyrB. The potency of novobiocin is considerably higher than that of the fluoroquinolones that also target DNA gyrase, but at a different site on the enzyme. The GyrA subunit is involved in the DNA nicking and ligation activity [1-4].
Olsalazine is an anti-inflammatory drug used in the treatment of Inflammatory Bowel Disease and Ulcerative Colitis.
Target: Antibacterial
Olsalazine is a derivative of salicylic acid. Inactive by itself (it is a prodrug), it is converted by the bacteria in the colon to mesalamine. Olsalazine is potent inhibitors of human intestinal macrophages chemotaxis to LTB4 with IC50 of 0.39 mM. Olsalazine (0.4 mM) inhibits the superoxide radical production generated by phorbol myristate acetate (PMA)-activated neutrophils or by xanthine-xanthine oxidase reaction by reduction of 31% and 73%, respectively. Olsalazine inhibits tumor growth in a rodent model of colorectal cancer. In 1,2-dimethylhydrazine-treated rats, Olsalazine (25 mg/kg/day) decreases number and volume of tumors by 58.17% and 62.67%, respectively. Administration of Olsalazine induces a 1.7-fold times increase in the number of apoptotic cells, companied with a reduction of 42.4% in cell proliferation rate.
Omadacycline is a new tetracycline antibiotic in the pipeline, which can inhibit the 30s subunit of bacterial ribosome.
IC50 Value:
Target: Antibacterial
in vitro:
in vivo:
Clinical trial: Phase III Study to Compare the Safety and Efficacy of PTK-0796 in Patients With Complicated Skin and Skin Structure Infection (CSSSI).
Omadacycline mesylate is a new tetracycline antibiotic in the pipeline, which can inhibit the 30s subunit of bacterial ribosome.
IC50 Value: N/A
Target: Antibacterial
in vitro:
in vivo:
Clinical trial: Phase III Study to Compare the Safety and Efficacy of PTK-0796 in Patients With Complicated Skin and Skin Structure Infection (CSSSI).
Omadacycline tosylate is a new tetracycline antibiotic in the pipeline, which can inhibit the 30s subunit of bacterial ribosome.
IC50 Value:
Target: Antibacterial
in vitro:
in vivo:
Clinical trial: Phase III Study to Compare the Safety and Efficacy of PTK-0796 in Patients With Complicated Skin and Skin Structure Infection (CSSSI).
Ornidazole(Ro 7-0207) is a 5-nitroimidazole derivative with antiprotozoal and antibacterial properties against anaerobic bacteria.
Target: Antibacterial; Antiparasitic
Ornidazole is a drug that cures some protozoan infections. Ornidazole 1 g/day is effective for the prevention of recurrence of Crohn's disease after ileocolonic resection [1]. Ornidazole is converted to reduction products that interact with DNA to cause destruction of helical DNA structure and strand leading to a protein synthesis inhibition and cell death in susceptible organisms [2].
Oxacillin sodium monohydrate is an antibiotic similar to flucloxacillin used in resistant staphylococci infections.
Target: Antibacterial
Oxacillin is a penicillinase-resistant β-lactam. It is similar to methicillin, and has replaced methicillin in clinical use. Another related compound is nafcillin. Since it is resistant to penicillinase enzymes, such as that produced by Staphylococcus aureus, it is widely used clinically in the US to treat penicillin-resistant Staphylococcus aureus. However, with the introduction and widespread use of both oxacillin and methicillin, antibiotic-resistant strains called oxacillin-resistant Staphylococcus aureus (MRSA/ORSA) have become increasingly prevalent worldwide. MRSA/ORSA is treated using vancomycin. From Wikipedia.
Oxytetracycline is a tetracycline analog isolated from the actinomycete streptomyces rimosus and used in a wide variety of clinical conditions.
Target: Antibacterial
Oxytetracycline was the second of the broad-spectrum tetracycline group of antibiotics to be discovered. Oxytetracycline works by interfering with the ability of bacteria to produce essential proteins. Without these proteins, the bacteria cannot grow, multiply and increase in numbers. Oxytetracycline therefore stops the spread of the infection and the remaining bacteria are killed by the immune system or eventually die.Oxytetracycline is a broad-spectrum antibiotic, active against a wide variety of bacteria. However, some strains of bacteria have developed resistance to this antibiotic, which has reduced its effectiveness for treating some types of infections [1, 2].
PA-824(Pretomanid) is a small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis; the MIC values of PA-824 against a panel of MTB pan-sensitive and rifampin mono-resistant clinical isolates ranged from 0.015 to 0.25 ug/ml.
IC50 value: 0.015 to 0.25 ug/ml (MICs) [1]
Target: tuberculosis
PA-824 exhibited a sub-micromolar minimal inhibitory concentration (MIC) against MTB, Although PA-824 was not the most potent NAP against cultured MTB clinical isolates, it was the most active in infected mice when orally administered at 25 mg kg -1. This indicated that PA-824 might possess more desirable pharmacokinetic properties than the other more potent NAP compounds that we tested. Further studies in mice at 25, 50 and 100 mg kg-1 PA-824 daily for 10 days resulted in reductions of mycobacterial burden in both spleen and lung tissues that were comparable to that of INH at 25 mg kg -1 [1]. PA-824 showed significant activity at 2, 10, and 50 microg/ml, similar to that of metronidazole, in a dose-dependent manner. PA-824 at 100 mg/kg in cyclodextrin/lecithin was as active as moxifloxacin at 100 mg/kg and isoniazid at 25 mg/kg and was slightly more active than rifampin at 20 mg/kg. Long-term treatment with PA-824 at 100 mg/kg in cyclodextrin/lecithin reduced the bacterial load below 500 CFU in the lungs and spleen [2]. PA-824 has no effect on the viability of M. leprae in all three models, consistent with the lack of the nitroimidazo-oxazine-specific nitroreductase, encoded by Rv3547 in the M. leprae genome, which is essential for activation of this molecule [3].
Pazufloxacin (T-3761) is a fluoroquinolone antibiotic.
Target: Antibacterial
Pazufloxacin (T-3761), a new quinolone derivative, showed broad and potent antibacterial activity. T-3761 showed good efficacy in mice against systemic, pulmonary, and urinary tract infections with gram-positive and gram-negative bacteria, including quinolone-resistant Serratia marcescens and Pseudomonas aeruginosa. The in vivo activity of T-3761 was comparable to or greater than those of ofloxacin, ciprofloxacin, norfloxacin, and tosufloxacin against most infection models in mice. The activities of T-3761 were lower than those of tosufloxacin against gram-positive bacterial systemic and pulmonary infections in mice but not against infections with methicillin-resistant Staphylococcus aureus [1]. T-3761 had a broad spectrum of activity and had potent activity against gram-positive and -negative bacteria. The MICs of T-3761 against 90% of the methicillin-susceptible Staphylococcus aureus, methicillin-susceptible and -resistant Staphylococcus epidermidis, and Clostridium spp. tested were 0.39 to 6.25 micrograms/ml. The MBCs of T-3761 were either equal to or twofold greater than the MICs. The 50% inhibitory concentrations of T-3761 for DNA gyrases isolated from E. coli and P. aeruginosa were 0.88 and 1.9 micrograms/ml, respectively [2].
Pefloxacin is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse).
Target: DNA gyrase
Pefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threatening bacterial infections. Pefloxacin is commonly referred to as afluoroquinolone (or quinolone) drug and is a member of the fluoroquinolone class of antibacterials. It is an analog of norfloxacin. It is a synthetic fluoroquinolone, belonging to the 3rd generation of quinolones. Pefloxacin is extensively prescribed in France. Pefloxacin has not been approved for use in the United States.
The bactericidal action of pefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.
Pefloxacin mesylate is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse).
Target: DNA gyrase
Pefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threatening bacterial infections. Pefloxacin is commonly referred to as afluoroquinolone (or quinolone) drug and is a member of the fluoroquinolone class of antibacterials. It is an analog of norfloxacin. It is a synthetic fluoroquinolone, belonging to the 3rd generation of quinolones. Pefloxacin is extensively prescribed in France. Pefloxacin has not been approved for use in the United States.
The bactericidal action of pefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.
Pefloxacin mesylate dehydrate is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse).
Target: DNA gyrase
Pefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threatening bacterial infections. Pefloxacin is commonly referred to as afluoroquinolone (or quinolone) drug and is a member of the fluoroquinolone class of antibacterials. It is an analog of norfloxacin. It is a synthetic fluoroquinolone, belonging to the 3rd generation of quinolones. Pefloxacin is extensively prescribed in France. Pefloxacin has not been approved for use in the United States.
The bactericidal action of pefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.
Protionamide (or prothionamide) is a drug used in the treatment of tuberculosis; has also been tested for use in the treatment of leprosy.
Target: Anti tuberculosis
Although ETH and PTH are both potent drugs against M. tuberculosis (MIC = ～0.5 μg/ml) (24), they do not affect E. coli growth, even at very high concentrations (100 μg/ml), which is primarily caused by the absence of an EthA homologue in E. coli [1]. Clinical improvement was noted in 74% of the patients treated with ethionamide and in 83% of those treated with prothionamide. Therapy was well tolerated and drug-related hepatotoxicity did not require discontinuation of therapy. The 500-mg dose of both ethionamide and prothionamide resulted in loss in Mycobacterium leprae viability more rapidly than did the 250-mg dose, and prothionamide at both dose levels was superior to the equivalent dose of ethionamide [2].
Prulifloxacin(NM441) is an older synthetic antibiotic of the fluoroquinolone drug class.
Target: Antibacterial
Prulifloxacin prevents bacterial DNA replication, transcription, repair and recombination through inhibition of bacterial DNA gyrase.
Pyrazinamide is a pyrazine that is used therapeutically as an antitubercular agent.
Target: Antibacterial
Pyrazinamide is a prodrug that stops the growth of Mycobacterium tuberculosis. Pyrazinoic acid was thought to inhibit the enzyme fatty acid synthase (FAS) I, which is required by the bacterium to synthesise fatty acids although this has been discounted. It was also suggested that the accumulation of pyrazinoic acid disrupts membrane potential and interferes with energy production, necessary for survival of M. tuberculosis at an acidic site of infection. Pyrazinoic acid binds to the ribosomal protein S1 (RpsA) and inhibits trans-translation. This may explain the ability of the drug to kill dormant mycobacteria [1-4].
Radezolid (RX-1741) is a novel oxazolidinone antibiotic agent.
IC50 Value:
Target: Anti-infection
Radezolid is a novel oxazolidinone antibiotic being developed by Rib-X Pharmaceuticals, Inc. for the treatment of serious multi-drug–resistant infections. Radezolid has completed two phase-II clinical trials. One of these clinical trials was for uncomplicated skin and skin-structure infections (uSSSI) and the other clinical trial was for community acquired pneumonia (CAP). From Wikipedia
Retapamulin(SB-275833) is a topical antibiotic, which binds to both E. coli and S. aureus ribosomes with similar potencies with Kd of 3 nM.
IC50 Value: 3 nM(Kd, E.coli)
Target: Antibacterial
Retapamulin is a topical antibiotic developed by GlaxoSmithKline. Retapamulin(SB-275833) is the first drug in the new class of pleuromutilin antibiotics to be approved for human use.Retapamulin(SB-275833) is marketed as an ointment under the brand names Altabax and Altargo. Retapamulin(SB-275833) is useful for Antibiotics.
Rifabutin(Mycobutin) is a semisynthetic ansamycin antibiotic with potent antimycobacterial properties.
IC50 Value:
Target: Antibacterial
Rifabutin is primarily bactericidal antibiotic drug used to treat tuberculosis. Its effect on bacteria is based on the DNA-dependent RNA polymerase blocking drug rifamycin S., a semi-synthetic derivative. It is effective, for example, in highly resistant mycobacteria, Gram-positive bacteria (and some are effective against Gram-negative bacteria), but also against Mycobacterium tuberculosis, M. leprae, and M. avium intracellulare.
Rifabutin is an antibiotic; antitumor. Rifabutin interferes with HSP-90 molecular chaperone, enhances ubiquitination and protein degradation, and inactivates bacterial RNA polymerase.
Rifampicin is a bactericidal antibiotic drug of the rifamycin group.
Target: Antibacterial
Rifampicin is a semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms [1, 2].
Rifapentine (Priftin; DL 473) is an antibiotic compound used in the treatment of tuberculosis.
Target: Antibacterial
Rifapentine inhibits DNA-dependent RNA polymerase activity in susceptible cells. Specifically, it interacts with bacterial RNA polymerase but does not inhibit the mammalian enzyme. A review of alternative regimens for prevention of active tuberculosis in HIV-negative individuals with latent TB found that a weekly, directly observed regimen of rifapentine with isoniazid for three months was as effective as a daily, self -administered regimen of isoniazid for nine months. But the rifapentine-isoniazid regimen had higher rates of treatment completion and lower rates of hepatotoxicity . However the rates of treatment-limiting adverse events were higher in the rifapentine-isoniazid regimen [1].
Rifaximin(Xifaxan) is an orally administered, semi-synthetic, nonsystemic antibiotic derived from rifamycin SV with antibacterial activity.
IC50 Value:
Target: RNA polymerase; antibacterial
Rifaximin is a semisynthetic, rifamycin-based non-systemic antibiotic, meaning that very little of the drug will pass the gastrointestinal wall into the circulation as is common for other types of orally administered antibiotics. It is used in the treatment of traveler's diarrhea and hepatic encephalopathy, for which it received orphan drug status from the U.S. Food and Drug Administration in 1998. Rifaximin interferes with transcription by binding to the β-subunit of bacterial RNA polymerase. This results in the blockage of the translocation step that normally follows the formation of the first phosphodiester bond, which occurs in the transcription process. From Wikipedia.
Roxithromycin is a semi-synthetic macrolide antibiotic.
Target: Antibacterial
Roxithromycin is a semi-synthetic macrolide antibiotic. It is used to treat respiratory tract, urinary and soft tissue infections. Roxithromycin is derived from erythromycin, containing the same 14-membered lactone ring. Roxithromycin prevents bacteria from growing, by interfering with their protein synthesis. Roxithromycin binds to the subunit 50S of the bacterial ribosome, and thus inhibits the translocation of peptides. Roxithromycin has similar antimicrobial spectrum as erythromycin, but is more effective against certain gram-negative bacteria, particularly Legionella pneumophila. From Wikipedia.
Salinomycin is an antibacterial and coccidiostat ionophore therapeutic drug.
IC50 Value:
Target: Antibacterial; Anticancer
Salinomycin, a polyether ionophore antibiotic isolated from Streptomyces albus, has been shown to kill CSCs in different types of human cancers, most likely by interfering with ABC drug transporters, the Wnt/β-catenin signaling pathway, and other CSC pathways[1].
in vitro: Salinomycin acts as a potassium ionophore and thereby interferes with transmembrane potassium potential, leading to mitochondrial and cellular potassium efflux. low concentrations of Salinomycin of 1 μM and 2 μM resulted in haggard and less confluent grown cells, increasing concentrations of Salinomycin of 5 μM and 10 μM resulted in a globular and defragmented cellular phenotype[2]. Treatment of 10.2 uM Sal for 48 h caused G0/G1 cell cycle arrest in HepG2 cells, whereas 15.3 uM Sal and 13.8 uM Sal for 48 h induced G2/M phase arrest in SMMC-7721 and BEL-7402 cells, respectively[3].
in vivo: After administration of 4 mg/kg Sal, 8 mg/kg Sal and 10 ul/g saline water for 6 weeks, the mice were sacrificed. The size of the liver tumors in the Sal treatment groups diminished compared with the control group. The mean diameter of the tumors decreased from 12.17 mm to 3.67 mm and the mean volume of the tumors decreased from 819 mm3 to 25.25 mm3 . Next, the tumors were harvested, followed by HE staining, immunohistochemistry, and TUNEL assays, to assess the anti-tumor activity of Sal in vivo[3].
Salinomycin is an antibacterial and coccidiostat ionophore therapeutic drug.
IC50 Value:
Target: Antibacterial; Anticancer
Salinomycin, a polyether ionophore antibiotic isolated from Streptomyces albus, has been shown to kill CSCs in different types of human cancers, most likely by interfering with ABC drug transporters, the Wnt/β-catenin signaling pathway, and other CSC pathways[1].
in vitro: Salinomycin acts as a potassium ionophore and thereby interferes with transmembrane potassium potential, leading to mitochondrial and cellular potassium efflux. low concentrations of Salinomycin of 1 μM and 2 μM resulted in haggard and less confluent grown cells, increasing concentrations of Salinomycin of 5 μM and 10 μM resulted in a globular and defragmented cellular phenotype[2]. Treatment of 10.2 uM Sal for 48 h caused G0/G1 cell cycle arrest in HepG2 cells, whereas 15.3 uM Sal and 13.8 uM Sal for 48 h induced G2/M phase arrest in SMMC-7721 and BEL-7402 cells, respectively[3].
in vivo: After administration of 4 mg/kg Sal, 8 mg/kg Sal and 10 ul/g saline water for 6 weeks, the mice were sacrificed. The size of the liver tumors in the Sal treatment groups diminished compared with the control group. The mean diameter of the tumors decreased from 12.17 mm to 3.67 mm and the mean volume of the tumors decreased from 819 mm3 to 25.25 mm3 . Next, the tumors were harvested, followed by HE staining, immunohistochemistry, and TUNEL assays, to assess the anti-tumor activity of Sal in vivo[3].
Sarafloxacin hydrochloride is a quinolone antibiotic drug.
Target: Antibacterial
sarafloxacin hydrochloride is a fluoroquinolone antibiotic registered for use against poultry diseases. Sarafloxacin treatment demonstrated mineralization to 14CO2 amounting to 0.58%, 0.49%, and 0.57% in loam, silt loam, and sandy loam soils, respectively, at the termination of the test [1]. The inhibitory level of sarafloxacin for the tested bacteria was strain dependent. It appeared that in broth culture Escherichia coli isolates were sensitive to sarafloxacin concentrations 5‐fold lower than the concentrations present in the simulated gut model, suggesting that sarafloxacin may be partially unavailable due to absorption to organic matter in the model [2]. Administering Sarafloxacin hydrochloride in the feed for 5 d at a dose of 10 or 12.5 mg/kg of fish proved efficacious in treating channel catfish infected with E. ictaluri in all three field trials. Average survival of the nonmedicated group was 43% in trial 1, 11°% in trial 2, and 59% in trial 3. Survival of the corresponding Sarafloxacin hydrochloride-medicated groups averaged 68, 48, and 73%. Antibiotic therapy with Sarafloxacin hydrochloride significantly (P < 0.05) improved survival in all trials [3].
Sitafloxacin is a new-generation, broad-spectrum oral fluoroquinolone antibiotic.
Target: Antibacterial
Sitafloxacin, a new-generation, broad-spectrum oral fluoroquinolone that is very active against many Gram-positive, Gram-negative and anaerobic clinical isolates, including strains resistant to other fluoroquinolones, was recently approved in Japan for the treatment of respiratory and urinary tract infections [1]. In terms of clinical efficacy, oral sitafloxacin was noninferior to oral levofloxacin in the treatment of community-acquired pneumonia or an infectious exacerbation of chronic respiratory tract disease, noninferior to oral tosufloxacin in the treatment of community-acquired pneumonia, and noninferior to oral levofloxacin in the treatment of complicated urinary tract infections, according to the results of randomized, double-blind, multicentre, noninferiority trials. Noncomparative studies demonstrated the efficacy of oral sitafloxacin in otorhinolaryngological infections, urethritis in men, C. trachomatis-associated cervicitis in women and odontogenic infections [2].
Sitafloxacin Hydrate is a new-generation, broad-spectrum oral fluoroquinolone antibiotic.
Target: Antibacterial
Sitafloxacin Hydrate, a new-generation, broad-spectrum oral fluoroquinolone that is very active against many Gram-positive, Gram-negative and anaerobic clinical isolates, including strains resistant to other fluoroquinolones, was recently approved in Japan for the treatment of respiratory and urinary tract infections [1]. In terms of clinical efficacy, oral sitafloxacin was noninferior to oral levofloxacin in the treatment of community-acquired pneumonia or an infectious exacerbation of chronic respiratory tract disease, noninferior to oral tosufloxacin in the treatment of community-acquired pneumonia, and noninferior to oral levofloxacin in the treatment of complicated urinary tract infections, according to the results of randomized, double-blind, multicentre, noninferiority trials. Noncomparative studies demonstrated the efficacy of oral sitafloxacin in otorhinolaryngological infections, urethritis in men, C. trachomatis-associated cervicitis in women and odontogenic infections [2].
Sparfloxacin is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity.
Target: Antibacterial
Sparfloxacin shows broad and potent antibacterial activity. Its MICs for 90% of the strains tested are 0.1 to 0.78 μg/ml against gram-positive organisms, such as members of the genera Staphylococcus , Streptococcus and Enterococcus , and 0.0125 to 1.56 μg/ml against gram-negative organisms, such as members of the family Enterobacteriaceae and the genera Pseudomona . Its MICs are 0.025 to 0.78 μg/ml against glucose nonfermenters, 0.2 to 0.78 μg/ml against anaerobes, 0.0125 to 0.05 μg/ml against Legionella. Sparfloxacin showed good oral efficacy against systemic infections with Staphylococcus aureus , Streptococcus pyogenes , Streptococcus pneumoniae , Escherichia coli , and Pseudomonas aeruginosa in mice [1]. Sparfloxacin targets DNA gyrase and inhibits DNA synthesis [2].
Spectinomycin Dihydrochloride is a new parenteral antibiotic prepared from Streptomyces spectabilis.
Target: Antibacterial
Spectinomycin is an antibiotic produced by Streptomyces spectabilis. It is active against gram-negative bacteria and used for the treatment of gonorrhea. Spectinomycin binds to the 30S subunit of the bacterial ribosome and interrupts protein synthesis. One form of resistance has emerged in the 16S ribosomal RNA in Pasteurella multocida [1]. It is given by injection to treat gonorrhea, especially in patients who are allergic to penicillins. A resistance-conferring gene for spectinomycin can also be used as a selection marker in bacteria for molecular cloning purposes. Furthermore, Spectinomycin is used as a selection agent for transformed plant cells that contain the selectable marker gene Spcr [2].
SQ109 is an orally active, small molecule antibiotic for treatment of pulmonary T(tuberculosis).
IC50 Value:
Target: Antibacterial
In Phase I clinical trials, SQ109 could replace one or more drugs in the current first-line TB drug regimen, simplify therapy, and shorten the TB treatment regimen. SQ109 has excellent in vitro activity against Mycobacterium tuberculosis within a MIC range of 1-0.5 μM (drug susceptible) and drug resistant TB bacteria, including XDR-TB, as well as potent in vivo activity against pulmonary TB alone and with other TB drugs.
Streptomycin is an aminoglycoside antibiotic produced by the soil actinomycete Streptomyces griseus.
Target: Antibacterial
Streptomycin sulfate is a sulfate salt of streptomycin that is a protein synthesis inhibitor. It binds to the small 16S rRNA of the 30S subunit of the bacterial ribosome, interfering with the binding of formyl-methionyl-tRNA to the 30S subunit. This leads to codon misreading, eventual inhibition of protein synthesis and ultimately death of microbial cells through mechanisms that are still not understood. Speculation on this mechanism indicates that the binding of the molecule to the 30S subunit interferes with 50S subunit association with the mRNA strand. This results in an unstable ribosomal-mRNA complex, leading to a frameshift mutation and defective protein synthesis; leading to cell death. Humans have structurally different ribosomes from bacteria, thereby allowing the selectivity of this antibiotic for bacteria. At low concentrations, however, Streptomycin only inhibits growth of the bacteria by inducing prokaryotic ribosomes to misread mRNA. Streptomycin is an antibiotic that inhibits both Gram-positive and Gram-negative bacteria, and is therefore a useful broad-spectrum antibiotic [1, 2].
Sulbactam(Betamaze) is an irreversible β-lactamase inhibitor.
Target: β-lactamase; Antibacterial
Sulbactam is a mechanism-based inhibitor of beta-lactamase enzymes used in clinical practice. sulbactam was the antimicrobial agent responsible for the killing of these organisms [1]. sulbactam may prove effective for non-life-threatening A. baumannii infections. Its role in the treatment of severe infections is unknown. However, the current formulation of sulbactam alone may allow its use at higher doses and provide new potential synergic combinations, particularly for those infections by A. baumannii resistant to imipenem [2].
Sulfacetamide Sodium is an anti-infective agent that is used topically to treat skin infections and orally for urinary tract infections.
Target: Antibacterial
Sulfacetamide is a sulfonamide antibiotic. Sulfacetamide is able to inhibit the growth of all isolated strains. Depending on the type of bacteria concentrations of 0.006 up to 6.4% sodium sulfacetamide proved to be effective. Simultaneously, all patients were treated with sulfacetamide containing ointment and/or eye drops 4 times daily for maximum of 14 days. With swabs taken at intervals of 7 and 14 days no bacterial growth was detected. Sulfacetamide 10% topical lotion, sold under the brand name Klaron or Ovace, is approved for the treatment of acne and seborrheic dermatitis. Sulfacetamide has been investigated for use in the treatment of pityriasis versicolor and rosacea. It may also have anti-inflammatory properties when used to treat blepharitis or conjunctivitis. It is believed to work by limiting the presence of folic acid which bacteria need to survive. It has been suggested that sulfacetamide may also serve as a treatment for mild forms of hidradenitis suppurativa. Sulfacetamide has antibacterial activity and is used to control acne. Some research indicates that sulfacetamide derivatives may act as antifungals by an CYP51A1-independent mechanism [1-4].
Sulfadiazine is a sulfonamide antibiotic.
Target: Antibacterial
Sulfadiazine eliminates bacteria that cause infections by stopping the production of folate inside the bacterial cell, and is commonly used to treat urinary tract infections (UTIs). In combination, sulfadiazine and pyrimethamine, can be used to treat toxoplasmosis, a disease caused by Toxoplasma gondii. From Wikipedia.
The ulcers who treated with silver sulfadiazine cream responded rapidly, with one-third showing bacterial levels of less than 10(5) within three days, and half within a week [1].
Sulfadimethoxine is a sulfonamide antibiotic.
Target: Antibacterial
Sulfadimethoxine is a sulfonamide antibiotic. Sulfadimethoxine is used to treat many infections including treatment of respiratory, urinary tract, enteric, and soft tissue infections. It is most frequently used in veterinary medicine, although it is approved in some countries for use in humans. Sulfadimethoxine inhibits bacterial synthesis of folic acid (pteroylglutamic acid) from para-aminobenzoic acid. Sulfadimethoxine is approved in Russia for use in humans, including children, and has been successfully used there for more than 35 years. It is widely available in Russia as an over-the-counter drug manufactured by a number of Russian pharmaceutical companies [1].
Sulfamerazine(RP-2632) is a sulfonamide antibacterial.
Target: Antibacterial
Sulfamerazine, the monomethyl derivative of sulfadiazine, is 2-sulfanilamido-4-methylpyrimidine. Sulfamerazine is a sulfonamide drug that inhibits bacterial synthesis of dihydrofolic acid by competing with para-aminobenzoic acid (PABA) for binding to dihydropteroate synthetase (dihydrofolate synthetase). Sulfamerazine is bacteriostatic in nature. Inhibition of dihydrofolic acid synthesis decreases the synthesis of bacterial nucleotides and DNA [1].
Sulfamerazine Sodium is a sulfonamide antibacterial.
Target: Antibacterial
Sulfamerazine, the monomethyl derivative of sulfadiazine, is 2-sulfanilamido-4-methylpyrimidine. Sulfamerazine is a sulfonamide drug that inhibits bacterial synthesis of dihydrofolic acid by competing with para-aminobenzoic acid (PABA) for binding to dihydropteroate synthetase (dihydrofolate synthetase). Sulfamerazine is bacteriostatic in nature. Inhibition of dihydrofolic acid synthesis decreases the synthesis of bacterial nucleotides and DNA [1].
Sulfameter(Bayrena) is a long-acting sulfonamide antibacterial.
Target: Antibacterial
Sulfameter(Bayrena) is a long-acting sulfonamide antibacterial. It is used as a leprostatic agent in the treatment of urinary tract infections.
Six physically healthy patients each were given 2 g of sulfameter simultaneously with a high lipid, high protein and high carbohydrate test meal. This experiment was designed as a threefold crossover study, and there was a randomized assignment of patients to the different conditions. The results show that sulfameter is significantly better absorbed when administered with a high lipid meal than when given with a high protein or high carbohydrate meal, demonstrated by the areas under the serum concentration curves (AUC), by the peak serum concentration and by the cumulative renal excretion.
Sulfamethazine is a sulfonamide antibacterial.
Target: Antibacterial
Sulfamethazine is an antibiotic used to treat bronchitis, prostatitis and urinary tract infections. Sulfamethazine blocks the synthesis of dihydrofolic acid by inhibiting dihydropteroate synthase. In addition, sulfamethazine is a structural analog and competitive antagonist of para-aminobenzoic acid (PABA) and can inhibit normal bacterial utilization of PABA for the synthesis of folic acid, which is an important metabolite in DNA synthesis [1, 2].
Sulfamethizole is a sulfathiazole antibacterial agent.
Target: Antibacterial
Sulfamethizole is a sulfathiazole antibacterial agent. Sulfamethizole is a competitive inhibitor of bacterial para-aminobenzoic acid (PABA), a substrate of the enzyme dihydropteroate synthetase. The inhibited reaction is necessary in these organisms for the synthesis of folic acid. Sulfamethizole, an inhibitor of dihydropteroate synthetase and the formation of folic acid, inhibited bioluminescence more than growth [1]. Treatment with sulfamethizole resulted in a significant reduction in bacterial counts in all samples from a susceptible strain (MIC, 128 micro g/ml) and a resistant strain (MIC, 512 micro g/ml). Infection with a sulII gene-positive strain (MIC, >2,048 micro g/ml) could not be treated with sulfamethizole, as no effect could be demonstrated in the urine, bladder, or kidneys [2].
Sulfamethoxazole is a sulfonamide bacteriostatic antibiotic.
Target: Antibacterial
Sulfonamides are structural analogs and competitive antagonists of para-aminobenzoic acid (PABA). They inhibit normal bacterial utilization of PABA for the synthesis of folic acid, an important metabolite in DNA synthesis. The effects seen are usually bacteriostatic in nature. Folic acid is not synthesized in humans, but is instead a dietary requirement. This allows for the selective toxicity to bacterial cells (or any cell dependent on synthesizing folic acid) over human cells. Bacterial resistance to sulfamethoxazole is caused by mutations in the enzymes involved in folic acid synthesis that prevent the drug from binding to it.
Sulfanilamide is a competitive inhibitor for bacterial enzyme dihydropteroate synthetase with IC50 of 320 μM.
Target: dihydropteroate synthetase; Antibacterial
Sulfanilamide containing the sulfonamide functional group displays inhibitory activity for dihydropteroate synthetase partially purified from Escherichia coli which normally uses para-aminobenzoic acid (PABA) for synthesizing the necessary folic acid acting as a coenzyme in the synthesis of purine, pyrimidine and other amino acids, exhibiting an IC 50 of 320 μM for dihydropteroate synthetasea and Km of 2.5 uM for PABA [1]. Sulfanilamide shows IC50 of 286.8 μg/mL for recombinant S. cerevisiae strains with wild-type FOL1 genes, but the single mutation 55Trp to 55Ala or 57Pro to 57Ser within the putative active site of the fungal DHPS confers resistance to Sulfanilamide with IC50 of >800 μg/mL [2]. Administration of Sulfanilamide with the dosage of 100 mg/kg/day is effective in the prevention of P. carinii infection in the immunosuppressed rat model. When the dosage of sulfaguanidine and Sulfanilamide reduced to 10 mg/kg/day, breakthrough P. carinii infection occurs in the rats [3].
Sulfapyridine(Dagenan) is a sulfonamide antibacterial.
Target: Antibacterial
Sulfapyridine(Dagenan) is a sulfonamide antibacterial. Sulfapyridine is not prescribed for the treatment in humans any more. However, it may be used to treat Linear IgA Disease. It is a good antibacterial drug, but its water solubility is very dependent on PH. Thus, there is a risk of crystallization within the bladder or urethra, which could lead to pain or blockage. The drug sulfasalazine is structurally one molecule of mesalamine linked to one molecule of Sulfapyridine with an azo bond [1].
Sulfathiazole Sodium is an organosulfur compound that has been used as a short-acting sulfa drug.
Target: Antibacterial
Sulfathiazole (20 μg/L) starts to be degraded between day 31 and day 38 in one of the two batch reactors containing different wastewater matrices. Sulfathiazole is degraded at a substantially faster rate than sulfamethoxazole or sulfamethazine in the nitrification process (S3) [1]. Recovery from spiked manure slurry samples is 64% for Sulfathiazole at pH 9. Sulfathiazole has acidity constant of pKa of 7.1and retention times (tR) of 7.8. S/N values for Sulfathiazole are above 100 at the 1 mg/kg level [2]. Sulfathiazole sorption to inorganic sorbents exhibits pronounced pH dependence consistent with sorbate speciation and sorbent charge properties. Sulfathiazole cations are most important for sorption to clay minerals, followed by neutral species [3].
Sulfisoxazole, a endothelin receptor antagonist, is a sulfonamide antibacterial with an oxazole substituent.
Target: Antibacterial; Endothelin Receptor
The sulfanilamide antibacterial agent sulfisoxazole was found to be a good endothelin receptor antagonist (IC50's of 0.60 microM and 22 microM for the ETA and ETB receptors, respectively) [1]. Sulfisoxazole is used to treat or prevent infections in many different parts of the body. It belongs to the group of medicines known as sulfonamide antibiotics. It works by preventing the growth of bacteria [2].
TBA-354 is a potent anti-tuberculosis compound; maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates.
IC50 value:
Target: Anti-tuberculosis agent
in vitro: TBA-354 is narrow spectrum and bactericidal in vitro against replicating and nonreplicating Mycobacterium tuberculosis, with potency similar to that of delamanid and greater than that of PA-824. TBA-354 maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates [1]. TBA-354 is 5 to 10 times more potent than PA-824, but selected mutants are cross-resistant to PA-824 and delamanid. TBA-354 is 2 to 4 times more potent than PA-824 when combined with bedaquiline, and when administered at a dose equivalent to that of PA-824, TBA-354 demonstrated superior sterilizing efficacy [2].
in vivo: TBA-354 has high bioavailability and a long elimination half-life. In vitro studies suggest a low risk of drug-drug interactions. Low-dose aerosol infection models of acute and chronic murine tuberculosis reveal time- and dose-dependent in vivo bactericidal activity that is at least as potent as that of delamanid and more potent than that of PA-824.
Tebipenem(LJC-11036) is a broad spectrum orally administered antibiotic; exhibits slow tight-binding inhibition at low micromolar concentrations versus the chromogenic substrate nitrocefin; Km and kcat values are 0.8 μM and 0.03 min(-1) for Blac.
Tebipenem Pivoxil is a novel oral carbapenem antibiotic.
Target: Antibacterial
Tebipenem is a broad spectrum orally administered antibiotic, from the carbapenem subgroup of beta-lactam antibiotics. It was developed as a replacement drug to combat bacteria that had acquired antibiotic resistance to commonly used antibiotics. Tebipenem is formulated as the ester tebipenem pivoxil due to the better absorption and improved bioavailability of this form. It has performed well in clinical trials for ear infection and looks likely to be further developed in future [1-3].
Torezolid (TR-701; tedizolid) is a novel oxazolidinone for gram-positive infections.
IC50 Value: 8.7 μM(MAO-A); 5.7 μM(MAO-B)
Target: Antibacterial
Tedizolid was reversible inhibitors of human MAO-A and MAO-B; the 50% inhibitory concentration (IC50) for tedizolid was 8.7 μM for MAO-A and 5.7 μM for MAO-B. Tedizolid phosphate was negative in the mouse head twitch model of serotonergic activity. Two randomized placebo-controlled crossover clinical studies assessed the potential of 200 mg/day tedizolid phosphate (at steady state) to enhance pressor responses to coadministered oral tyramine or pseudoephedrine. Sensitivity to tyramine was determined by comparing the concentration of tyramine required to elicit a ≥ 30-mmHg increase in systolic blood pressure (TYR30) when administered with placebo versus tedizolid phosphate. The geometric mean tyramine sensitivity ratio (placebo TYR30/tedizolid phosphate TYR30) was 1.33; a ratio of ≥ 2 is considered clinically relevant. In the pseudoephedrine study, mean maximum systolic blood pressure was not significantly different when pseudoephedrine was coadministered with tedizolid phosphate versus placebo.
Telithromycin(HMR3647) is a ketolide antibiotic to treat community acquired pneumonia of mild to moderate severity.
Target: Antibacterial
Telithromycin prevents bacteria from growing, by interfering with their protein synthesis. Telithromycin binds to the subunit 50S of the bacterial ribosome, and blocks the progression of the growing polypeptide chain. Telithromycin has over 10 times higher affinity to the subunit 50S than erythromycin. In addition, telithromycin strongly bind simultaneously to two domains of 23S RNA of the 50 S ribosomal subunit, where older macrolides bind strongly only to one domain and weakly to the second domain. Telithromycin can also inhibit the formation of ribosomal subunits 50S and 30S. From Wikipedia.
Tetracycline is a broad spectrum polyketide antibiotic.
Target: Antibacterial
Tetracycline is a broad spectrum polyketide antibiotic produced by the Streptomyces genus of Actinobacteria. It exerts a bacteriostatic effect on bacteria by binding reversible to the bacterial 30S ribosomal subunit and blocking incoming aminoacyl tRNA from binding to the ribosome acceptor site. It also binds to some extent to the bacterial 50S ribosomal subunit and may alter the cytoplasmic membrane causing intracellular components to leak from bacterial cells [1].
Thiamphenicol is an antimicrobial antibiotic and a methyl-sulfonyl analogue of chloramphenicol.
Target: Antibacterial
Thiamphenicol (also known as thiophenicol and dextrosulphenidol) is an antibiotic. It is the methyl-sulfonyl analogue of chloramphenicol and has a similar spectrum of activity, but is 2.5 to 5 times as potent. Like chloramphenicol, it is insoluble in water, but highly soluble in lipids. It is used in many countries as a veterinary antibiotic, but is available in China, Morocco and Italy for use in humans. Its main advantage over chloramphenicol is that it has never been associated with aplastic anaemia. Thiamphenicol is a derivative of chloramphenicol characterized by a spectrum comparable to that of the parent compound against multiresistant pathogens but showing satisfactory tolerability. Thiamphenicol showed a significant PAE (0.33 to 2.9h) on all pathogens studied and a powerful bactericidal effect against beta-lactamase-positive and -negative H. influenzae. These results indicate a good in vitro activity of thiamphenicol against difficult-to-treat multiply resistant pathogens [1, 2].
Tigecycline is a first-in-class, broad spectrum antibiotic with activity against antibiotic-resistant organisms.
Target: Antibacterial
Tigecycline is active against a broad range of gram-negative and gram-positive bacterial species including clinically important multidrug-resistant nosocomial and community-acquired bacterial pathogens. Tigecycline has been shown to inhibit the translation elongation step by binding to the ribosome 30S subunit and preventing aminoacylated tRNAs to accommodate in the ribosomal A site [1]. Tigecycline has also been found to be effective for the treatment of community- as well as hospital-acquired and ventilator-associated pneumonia and bacteremia, sepsis with shock and urinary tract infections. Tigecycline appears to be a valuable treatment option for the management of superbugs, especially where conventional therapy has failed [2].
Fifteen patients received tigecycline for 16 episodes of CPKP infection. The main infections were pneumonia (31%), urinary tract infection (31%), peritonitis (20%), catheter-related bacteraemia (12%), and meningitis (6%). Most infections were complicated with severe sepsis (44%), septic shock (12%), and/or bacteraemia (19%). The daily maintenance dose of tigecycline was 200 mg in 10 episodes and 100 mg in 6 episodes. The overall 30-day mortality rate was 25%. Univariate analysis showed that mortality was significantly associated (p < 0.01) with mean APACHE II and SOFA scores and the presence of immunosuppression, but not with the tigecycline dose [3].
Clinical indications: Acinetobacter infection; Bacterial infection; Bacterial pneumonia; Bacterial skin infection; Bacteroides fragilis infection; Bacteroides infection; Citrobacter infection; Clostridiaceae infection; Clostridium difficile infection; Clostridium infection; Enterobacter infection
FDA Approved Date: June 17, 2005
Toxicity: nausea; vomiting; diarrhea; local IV-site reaction; infection; fever; headache
Tigecycline hydrochloride is a first-in-class, broad spectrum antibiotic with activity against antibiotic-resistant organisms.
Target: Antibacterial
Tigecycline hydrochloride is active against a broad range of gram-negative and gram-positive bacterial species including clinically important multidrug-resistant nosocomial and community-acquired bacterial pathogens. Tigecycline hydrochloride has been shown to inhibit the translation elongation step by binding to the ribosome 30S subunit and preventing aminoacylated tRNAs to accommodate in the ribosomal A site [1]. Tigecycline hydrochloride has also been found to be effective for the treatment of community- as well as hospital-acquired and ventilator-associated pneumonia and bacteremia, sepsis with shock and urinary tract infections. Tigecycline hydrochloride appears to be a valuable treatment option for the management of superbugs, especially where conventional therapy has failed [2].
Fifteen patients received tigecycline hydrochloride for 16 episodes of CPKP infection. The main infections were pneumonia (31%), urinary tract infection (31%), peritonitis (20%), catheter-related bacteraemia (12%), and meningitis (6%). Most infections were complicated with severe sepsis (44%), septic shock (12%), and/or bacteraemia (19%). The daily maintenance dose of tigecycline hydrochloride was 200 mg in 10 episodes and 100 mg in 6 episodes. The overall 30-day mortality rate was 25%. Univariate analysis showed that mortality was significantly associated (p < 0.01) with mean APACHE II and SOFA scores and the presence of immunosuppression, but not with the tigecycline hydrochloride dose [3].
Clinical indications: Acinetobacter infection; Bacterial infection; Bacterial pneumonia; Bacterial skin infection; Bacteroides fragilis infection; Bacteroides infection; Citrobacter infection; Clostridiaceae infection; Clostridium difficile infection; Clostridium infection; Enterobacter infection
FDA Approved Date: June 17, 2005
Toxicity: nausea; vomiting; diarrhea; local IV-site reaction; infection; fever; headache
Tigecycline mesylate a first-in-class, broad spectrum antibiotic with activity against antibiotic-resistant organisms.
Target: Antibacterial
Tigecycline mesylate is active against a broad range of gram-negative and gram-positive bacterial species including clinically important multidrug-resistant nosocomial and community-acquired bacterial pathogens. Tigecycline mesylate has been shown to inhibit the translation elongation step by binding to the ribosome 30S subunit and preventing aminoacylated tRNAs to accommodate in the ribosomal A site [1]. Tigecycline mesylate has also been found to be effective for the treatment of community- as well as hospital-acquired and ventilator-associated pneumonia and bacteremia, sepsis with shock and urinary tract infections. Tigecycline mesylate appears to be a valuable treatment option for the management of superbugs, especially where conventional therapy has failed [2].
Fifteen patients received tigecycline mesylate for 16 episodes of CPKP infection. The main infections were pneumonia (31%), urinary tract infection (31%), peritonitis (20%), catheter-related bacteraemia (12%), and meningitis (6%). Most infections were complicated with severe sepsis (44%), septic shock (12%), and/or bacteraemia (19%). The daily maintenance dose of tigecycline mesylate was 200 mg in 10 episodes and 100 mg in 6 episodes. The overall 30-day mortality rate was 25%. Univariate analysis showed that mortality was significantly associated (p < 0.01) with mean APACHE II and SOFA scores and the presence of immunosuppression, but not with the tigecycline mesylate dose [3].
Clinical indications: Acinetobacter infection; Bacterial infection; Bacterial pneumonia; Bacterial skin infection; Bacteroides fragilis infection; Bacteroides infection; Citrobacter infection; Clostridiaceae infection; Clostridium difficile infection; Clostridium infection; Enterobacter infection
FDA Approved Date: June 17, 2005
Toxicity: nausea; vomiting; diarrhea; local IV-site reaction; infection; fever; headache
Tildipirosin(Zuprevo) is a novel 16-membered macrolide for treatment, control, and prevention of bovine respiratory disease; inhibits protein synthesis on the ribosome (IC50= 0.23 ± 0.01 μM).
IC50 value:
Target: Antibiotic; Protein synthesis inhibitor
The efficacy of tildipirosin at inhibiting protein synthesis on the ribosome is 50% inhibitory concentration [IC(50)], 0.23 ± 0.01 μM [1]. The time-concentration profile of tildipirosin in BF and lung far exceeded that in blood plasma. In lung, tildipirosin concentrations reached 3.1 μg/g at 2 h, peaked at 4.3 μg/g at day 1, and slowly declined to 0.8 μg/g at day 17. In BF, tildipirosin levels were 14.3, 7.0, and 6.5 μg/g at days 5, 10, and 14. T1/2 in lung was ～7 days. Tildipirosin is rapidly and extensively distributed to the respiratory tract followed by slow elimination [2].
Tinidazole is a synthesized imidazole derivative used in antiprotozoal treatment with antiamebic and antibacterial properties.
Target: Antibacterial
Tinidazole is a 5-nitroimidazole active in vitro against a wide variety of anaerobic bacteria and protozoa. Tinidazole is an effective treatment against anaerobic microorganisms based on its pharmacokinetic characteristics (C(max) 51 microg/ml, t(1/2) 12.5 h) and its excellent in vitro activity. Its long half-life allows once a day regimens. Tinidazole is as effective as metronidazole in the treatment of infections caused by T. vaginalis, giardiasis and amebiasis and bacterial vaginosis, malaria, odontogenic infections, anaerobic bacterial infections (pelvic inflammatory disease, diabetic foot), surgical prophylaxis (abdominal and hysterectomy) and Helicobacter pylori eradication.
Tinidazole has recently been resurrected and FDA approved for trichomoniasis and BV in the USA and is being restudied as an alternative to metronidazole for BV. In vitro antimicrobial activity and pharmacokinetics studies indicate that when compared directly with metronidazole, tinidazole has minor but possibly relevant antimicrobial as well as pharmacokinetic advantages.
Tobramycin is an aminoglycoside, broad-spectrum antibiotic produced by Streptomyces tenebrarius.
Target: Antibacterial
Tobramycin is an aminoglycoside antibiotic derived from Streptomyces tenebrarius and used to treat various types of bacterial infections, particularly Gram-negative infections. It is especially effective against species of Pseudomonas [1].
Tobramycin works by binding to a site on the bacterial 30S and 50S ribosome, preventing formation of the 70S complex. As a result, mRNA cannot be translated into protein and cell death ensues. Tobramycin is preferred over gentamicin for Pseudomonas aeruginosa pneumonia due to better lung penetration. From Wikipedia [2].
Tulathromycin A is a macrolide antibiotic.
IC50 Value: 1 microg/ml (MIC90 for Pasteurella multocida) [2]
Target: Antibacterial
in vitro: Two highly pathogenic strains of M. bovis (with minimum inhibitory concentration values for tulathromycin of 1 and >64 microg/ml) were inoculated into 145 calves. Four days after inoculation, calves with clinical BRD were treated subcutaneously with saline or tulathromycin (2.5 mg/kg). Compared with saline, BRD-related withdrawals, peak rectal temperatures, and lung lesion scores were significantly lower for tulathromycin-treated calves (P < .01). Tulathromycin was highly effective in the treatment of BRD due to M. bovis in calves regardless of the minimum inhibitory concentration of the challenge strain (1 or >64 microg/ml) [1]. The lowest concentrations inhibiting the growth of 90% of isolates (MIC90) for tulathromycin were 2 microg/ml for Mannheimia (Pasteurella) haemolytica, 1 microg/ml for Pasteurella multocida (bovine), and 2 microg/ml for Pasteurella multocida (porcine) and ranged from 0.5 to 4 microg/ml for Histophilus somni (Haemophilus somnus) and from 4 to 16 microg/ml for Actinobacillus pleuropneumoniae [2].
in vivo: Each study randomly allocated 250 calves to receivetulathromycin at 2.5 mg/kg and 250 calves to receive either tilmicosin at 10 mg/kg (Colorado site) or florfenicol at 40 mg/kg (Idaho and Texas sites) on arrival at the feedlot. Calves were housed by treatment group in pens with 50 calves/pen [3]. The treatment groups were physiologic saline (n = 160) given SC at 0.02 ml/kg, tulathromycin (n = 320) given SC at 2.5 mg/kg, and tilmicosin (n = 320) given SC at 10 mg/kg [4].Tulathromycin is a triamilide antimicrobial that has been approved for use in the treatment and prevention of bovine respiratory disease and the treatment of swine respiratory disease.
Toxicity: No adverse events related to tulathromycin were reported [4].
Clinical trial:
Tylosin (Fradizine; Tylocine; Tylosin A) is a broad spectrum antibiotic against Gram-positive organisms and a limited range of Gram-negative organisms
Tylosin phosphate(Fradizine; Tylocine; Tylosin A) is a broad spectrum antibiotic against Gram-positive organisms and a limited range of Gram-negative organisms.
Tylosin Tartrate is an antibiotic with a large macrocyclic lactone ring.
Target: Antibacterial
Tylosin is a bacteriostat food additive used in veterinary medicine. It has a broad spectrum of activity against gram-positive organisms and a limited range of gram-negative organisms. There is no significant evidence that tylosin resistant staphylococci of animal origin have endangered human health. Tylosin is not effective against the gram-negative intestinal flora, which thus does not lead to selection of R-factors by conjugation. From the human medical stand point, there is no reason that precludes the use of tylosin as a fee additive in animal feeds [1]. Minimum inhibitory concentrations for tylosin tartrate and other commonly used antibiotics were determined for 103 isolates. Most (82.61%) of the isolates not exposed to antibiotics in the 3 months before submission were sensitive to tylosin tartrate. These findings suggest that tylosin tartrate warrants further study as a first-line option for the treatment of dogs initially presenting with pyoderma [2].
Vancomycin (Vancocin) is an antibiotic useful for the treatment of a number of bacterial infections; is effective mostly against Gram-positive bacteria.
MICs value:
Vancomycin is a glycopeptide antibiotic which primarily used for the treatment of serious infections caused by Gram-(+) bacteria known or suspected to be resistant to other antibiotics.Orally administered vancomycin is recommended as a treatment for intestinal infection with Clostridium difficile, a common side effect of treatment with broad-spectrum antibiotics.
Vancomycin hydrochloride is a hydrochloride of vancomycin that is a narrow-spectrum glycopeptide antibacterial agent.
IC50 Value:
Target: Antibacterial
Vancomycin hydrochloride is a glycopeptide antibiotic that interferes with cell wall synthesis. Effective against Gram-positive bacteria. Vancomycin is a glycopeptide antibiotic that blocks bacterial cell wall biosynthesis at the level of peptidoglycan biosynthesis. It inhibits incorporation of terminal D-alanyl-D-alanine moieties of the NAM/NAG-peptides. It is effective against Gram-positive bacteria. Vancomycin also alters bacterial-cell-membrane permeability and RNA synthesis.
Walrycin B is a novel antibacterial compound specifically targeting the essential WalR response regulator.
IC50 value: 0.39 ug/ml (MIC for B. subtilis 168); 3.13 ug/ml (MIC for S. aureus N315) [1]
Target: bacterial WalR response regulator; Antibacterial
Walrycin B is known as an analog of toxoflavin (a phytotoxin from Burkholderia glumae), which has been shown to have a strong MIC for B. subtilis and S. aureus but whose mode of action is not clear. The compound could also interact with WalR to cause bactericidal effects.
Walrycins are a new class of potent small molecule compounds that kill bacterial cells by targeting the RR WalR and inhibiting this essential signal transduction pathway. They not only have therapeutic potential but will also prove to be useful reagents for the further study of the WalK/WalR TCS. Walrycin B target WalR and
lead to cell death in both B. subtilis and S. aureus.
Ofloxacin is a fluoroquinolone whose primary mechanism of action is inhibition of bacterial DNA gyrase.
Target: DNA gyrase
Ofloxacin is a fluoroquinolone whose primary mechanism of action is inhibition of bacterial DNA gyrase. In vitro it has a broad spectrum of activity against aerobic Gram-negative and Gram-positive bacteria, although it is poorly active against anaerobes [1]. Ofloxacin, like other 4-quinolones, is unusual among front line drugs available to treat bacterial infections since it affects bacterial DNA synthesis, rather than cell wall or protein synthesis [2].
Ofloxacin (20 mg/kg), norfloxacin (40 mg/kg), pefloxacin mesylate dihydrate (40 mg/kg)and ciprofloxacin (50 mg/kg) were administered by gavage twice daily for three consecutive weeks. 6 weeks after treatment, the test animals were euthanised and Achilles tendon specimens were collected. A computer monitored tensile testing machine was utilised for biomechanical testing. The mean elastic modulus of the control group was significantly higher than that of the norfloxacin and pefloxacin groups (p<0.05 and p<0.01, respectively). The mean yield force (YF) of the control group was significantly higher than those of ciprofloxacin, norfloxacin and pefloxacin groups (p<0.001, p<0.05 and p<0.01, respectively). The mean ultimate tensile force (UTF) of the control group was significantly higher than of the ciprofloxacin, norfloxacin, and pefloxacin groups (p<0.001, p<0.05 and p<0.01, respectively). Hyaline degeneration and fibre disarrangement were observed in the tendons of the ciprofloxacin, pefloxacin, and ofloxacin treated-groups, whereas myxomatous degeneration was observed only in the ciprofloxacin and pefloxacin groups [3].
Clinical indications: Bacterial infection; Bacterial respiratory tract infection; Bacterial urinary tract infection
Toxicity: tendinopathy; hepatotoxicity; dysglycemia
[1]. Todd PA, et al. Ofloxacin. A reappraisal of its antimicrobial activity, pharmacology and therapeutic use. Drugs. 1991 Nov;42(5):825-76.
[2]. Smith JT, et al. Ofloxacin, a bactericidal antibacterial. Chemotherapy. 1991;37 Suppl 1:2-13.
[3]. Olcay E, et al. Oral toxicity of pefloxacin, norfloxacin, ofloxacin and ciprofloxacin: comparison of biomechanical and histopathological effects on Achilles tendon in rats. J Toxicol Sci. 2011 Jun;36(3):339-45.
| M.Wt | 361.37 | Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
|---|---|---|---|
| Formula | C18H20FN3O4 | ||
| CAS No | 82419-36-1 | ||
| Solubility | DMSO 0.4 mg/mL; Water <1 mg/mL |
Products are for research use only. Not for human use. We do not sell to patients.
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