Infection

Tricyclazole-d₃ is the deuterium labeled Tricyclazole. Tricyclazole is a pentaketide-derived melanin biosynthesis inhibitor.

Cilastatin ammonium salt is an antibiotic that is relatively effective against Gram-positive cocci with a half-life of 3-4 h.

FtsZ-IN-5 is a potent FtsZ inhibitor, to promote FtsZ polymerization and inhibit GTPase activity of FtsZ. Thus, FtsZ-IN-5 inhibits bacterial division to lead to death of bacterial cells. FtsZ-IN-5 shows bactericidal activity with no significant tendency to trigger bacterial resistance as well as rapid bactericidal properties. And FtsZ-IN-5 shows low hemolytic activity and cytotoxicity to mammalian cells.

Anti-MRSA agent 3 (compound 18) has highly inhibitory activity against Methicillin-resistant Staphylococcus aureus (MRSA) with MIC of 0.098 μg/ml, and low cytotoxicity in normal cells. Anti-MRSA agent 3 has relatively strong ability to destroy bacterial cell wall and membrane, high binding affinity to bacterial genomic DNA.

Antifungal agent 11 shows the promising antifungal activity.

Protein kinase G inhibitor-2 (Compound 266) is a mycobacterial protein kinase G inhibitor, with an IC₅₀ of 3 μM. Protein kinase G inhibitor-2 can be used for mycobacterial infection research.

NBTIs-IN-5 (Compound 5r) is a NBTI (Novel Bacterial Topoisomerase Inhibitor) DNA gyrase inhibitor with an IC₅₀ of 1.5 μM against Mycobacterium abscessus (Mabs) DNA gyrase. NBTIs-IN-5 inhibits Mabs bamboo bacterial growth with an MIC₉₀ of 0.4 μM.

NEMURI is an antimicrobial peptide with sleep-promoting effect.

Moroxydine hydrochloride-d₈ (ABOB hydrochloride-d₈) is the deuterium labeled Moroxydine (ABOB) hydrochloride (HY-B0420A). Moroxydine hydrochloride is a broad-spectrum agent with multi-antiviral activities against DNA and RNA viruses, including influenza virus, herpes simplex, varicella zoster, measles, mumps disease, hepatitis C virus, etc. Moroxydine hydrochloride exhibits excellent antiviral activity and shows low cytotoxicity to cells infected by dsRNA viruses (grass carp reovirus, GCRV) and large DNA viruses (giant salamander iridovirus, GSIV). Moroxydine hydrochloride blocks the GCRV-induced cytopathic effects and eliminates nucleocapsids in ctenopharyngodon idella kidney (CIK) cells to keep the normal morphological structure. Moroxydine hydrochloride significantly inhibits the apoptosis, the caspase 3 activity, Bax expression and down-regulates Bcl-2 levels^[1][2][3].

Bipolaricin R (Compound 6) is a compound that can be isolated from Bipolaris maydis. Bipolaricin R exhibits noticeable antimicrobial ability against Bacillus cereus, Staphylococcus aureus, and Staphylococcus epidermidis. Bipolaricin R has excellent antiproliferation and apoptosis induction effects against A549 cell line.

ClpP1P2-IN-1 is a protease inhibitor targeting ClpP1P2 of Mycobacterium tuberculosis, with a K_i value of 0.04 μM. ClpP1P2-IN-1 inhibits the growth of Mycobacterium tuberculosis and shows low cytotoxicity against mammalian kidney cells. ClpP1P2-IN-1 can be used in the research of tuberculosis.

3′,4′,5′,5,6,7-Hexamethoxyflavone is a flavonoid with antiprotozoal activity. 3′,4′,5′,5,6,7-Hexamethoxyflavone inhibits trypanosoma bruceirhodesiense with IC₅₀ of 21.3 μM (8.58 g/mL).

Ilicicolin C exhibits antibacterial activity against Pseudomonas syringae with IC₅₀ of 28.5 µg/mL. Ilicicolin C exhibits weak inhibitory activities against acetylcholinesterase (AChE) and β-glucuronidase with IC₅₀ of 30-43 µg/mL. Ilicicolin C exhibits weak cytoxicity in human lung fibroblasts with IC₅₀ of 64-120 µg/mL. Ilicicolin C affects seed germination and root tip growth of lettuce.

Tachyplesin-3 is a broad-spectrum cationic antimicrobial peptide. Tachyplesin-3 has inhibitory activity against Gram-positive bacteria, Gram-negative bacteria, fungi and enveloped viruses. Tachyplesin-3 binds to bacterial membrane lipopolysaccharides through positive charges, disrupting membrane integrity and causing leakage of cellular contents. Tachyplesin-3 interferes with bacterial adhesion and aggregation, prevents biofilm formation, and has a synergistic effect when used in combination with Piperacillin (HY-B1923) - Tazobactam (HY-B1418) (TZP).

SB-734117 is a human cytomegalovirus (HCMV) replication inhibitor that prevents CREB and histone H3 post-translational modifications.

KOS-2079 is an antifungal agent. KOS-2079 has strong inhibitory activity against Aspergillus flavus 204303 (MIC = 1.10 μg/mL) and Aspergillus fumigatus 204305 (MIC = 1.32 μg/mL). KOS-2079 is commonly used in the study of fungal infection.

Ethambutol-d₄ dihydrochloride is deuterated labeled Ethambutol dihydrochloride (HY-B0535A). Ethambutol dihydrochloride is an antimycobacterial compound that prevents cell wall formation by inhibiting arabinosyltransferase activity.

GA-O-02, a 18β-Glycyrrhetinic acid derivative, is a potent antimicrobial and anti-inflammatory agent. GA-O-02 exerts anti-inflammation through the inhibition of NO, pro-inflammatory cytokines and chemokines. GA-O-02 displays a high antimicrobial activity against Gram-positive bacteria.

KLK6-IN-2 is a reversible non-covalent and selective KLK6 inhibitor, with an IC₅₀ of 2.1 μM against hKLK6. KLK6-IN-2 acts as a reversible competitive inhibitor of boar Spermatozoa acrosin, with a K_i of 2.6 μM against porcine acrosin. KLK6-IN-2 exhibits trypanocidal activity against Trypanosoma brucei rhodesiense, with an IC₅₀ of 3.71 μM.

Antileishmanial agent-7 (compound 23) is a potent antileishmanial agent. Antileishmanial agent-7 shows antileishmanial activity against Leishmania donovani and L-6, with IC₅₀ values of 6.89 and 259 μM, respectively.