Infection

Netivudine is a nucleoside analogue with potent anti-varicella zoster virus activity. Netivudine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

NSC 288387 is a pan-flavivirus MTase inhibitor. NSC 288387 binds to the SAM-binding pocket. NSC 288387 inhibits ZIKV with an IC₅₀ of 0.2 μM. NSC 288387 also inhibits viral replication in cell culture.

Alalevonadifloxacin (WCK-2349) mesylate is an orally active antibiotic targeting Gram-positive and Gram-negative bacteria. Alalevonadifloxacin mesylate is promising for research of acute bacterial skin and skin structure infections and hospital-acquired pneumonia caused by MRSA and other pathogens.

Paulomycin A (Volonomycin A) has anti-Gram-positive bacteria effect, and it has inhibitory effect on Staphylococcus aureus resistant to penicillin, Streptomycin, Neomycin and Macrolide antibiotics.

Fosamprenavir-d₄ is the Deuterium-labeled Fosamprenavir (HY-78726). Fosamprenavir is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir can be used for the study of human immunodeficiency virus (HIV-1) infection.

PSI 352707 (GS-566500) is a sofosbuvir metabolite with activity similar to other antiviral compounds. PSI 352707 showed good safety and tolerability in inhibiting chronic hepatitis C virus infection.

Isoxadifen-ethyl is a Herbicide safener that reduces herbicide toxicity to crops. Isoxadifen-ethyl enhances maize tolerance to Nicosulfuron (HY-B1876) by regulating detoxification gene expression; it reduces the phytotoxicity and damage induced by Cyhalofop-butyl (HY-B0861) in rice. Isoxadifen-ethyl is applicable to herbicide-related research.

Antimicrobial peptide 6b is a cationic macrocyclic antimicrobial peptide. It exhibits broad-spectrum antibacterial and antifungal activities, with a MIC of 1.5-6.2 μg/mL against drug-resistant Gram-positive bacteria, a MIC of 4-25 μg/mL against Gram-negative bacteria, and also shows activity against pathogenic fungi. It acts through a membrane disruption mechanism, has a unique "sandwich" conformation, low hemolytic activity, and can rapidly kill bacteria and eliminate bacterial and fungal biofilms. Antimicrobial peptide 6b can be used in studies of drug-resistant bacterial infections and fungal infections.

Anti-MRSA agent 20 (Compound a4) is an anti-microbial agent (MIC: < 0.03125 μg/mL) against MRSA). Anti-MRSA agent 20 binds to the ribosomal peptidyl transferase center and inhibits bacterial survival by inhibiting MRSA toxin synthesis and bacterial division. Anti-MRSA agent 20 significantly reduces the MRSA load in the lungs and attenuates lung injury in the MRSA-infected mice (ED₅₀ = 6.48 mg/kg).

K-252b, an indolocarbazole isolated from the actinomycete Nocardiopsis, is a PKC inhibitor. K-252b can be used to inhibit extracellular kinases of cells in culture because it can’t pass through cell membrane freely .

Antibiotic adjuvant 1 (compound 3e) is an antibiotic adjuvant that presents insufficient antibacterial activity (MIC > 128 µg/mL) and potentiate the activity of Cloxacillin (HY-B0466A)(66-fold) with synergistic effect.

2-Deethoxy-2-hydroxyphantomolin, Germacranolide, is an Antifungal and Antibacterial agent. 2-Deethoxy-2-hydroxyphantomolin can be isolated from Elephantopus tomentosus Linn and E. mollis. 2-Deethoxy-2-hydroxyphantomolin is moderately active against Candida albicans (14 mm clearing zone) and slightly active against Escherichia coli (12 mm), Pseudomonas aeruginosa (12 mm), Bacillus subtilis (14 mm), and Trichophyton mentagrophytes (13 mm).

MERS-CoV-IN-4 is an orally active antiviral inhibitor targeting the MERS-CoV spike (S) protein, with an IC₅₀ of 0.009 μM in Huh-7 cells, and K_d values of 7.72 μM for the full-length S protein and 5.09 μM for S-RBD. MERS-CoV-IN-4 inhibits viral entry, and suppresses MERS-CoV pseudoviruses and live viruses in vitro. MERS-CoV-IN-4 reduces pulmonary viral loads in hDPP4 transgenic mice. MERS-CoV-IN-4 can be used for research on Middle East respiratory syndrome coronavirus infection.

SARS-CoV-2-IN-96 (compound 12b) is an inhibitor of HCoV-OC43 (EC₅₀= 97 nM) and SARS-CoV-2 (EC₅₀= 45 nM) and low cytotoxicity (CC₅₀> 10 μM) in Huh7 cells.

HIV-1 protease-IN-7 (compound 16) is an orally active HIV-1 protease inhibitor (IC₅₀=3.52 nM, EC₅₀=37 nM).

Famotidine-¹³C₃ (MK-208-¹³C₃) is the ¹³C₃-labeled Famotidine (HY-B0377). Famotidine (MK-208) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer.

Antibacterial agent 107 (compound 14) is a potent antibacterial agent. Antibacterial agent 107 shows potent antibacterial activity against Gram-positive bacteria, with a MIC of 1.56 μg/mL (MRSA). Antibacterial agent 107 exhibits low hemolytic activity, high membrane selectivity, and rapid bactericidal activity. Antibacterial agent 107 shows effective in vivo efficacy in the murine model of bacterial keratitis caused by Staphylococcus aureus ATCC29213.

Antimalarial agent 27 (compound 11a) is an antimalarial agent, potently targeting to P.falciparum (IC₅₀=0.37 μM). Antimalarial agent 27 acts function via P.falciparum DXR (1-deoxy-D-xylulose-5-phosphate reductoisomerase) inhibition (IC₅₀=0.11 μM).

Tenofovir-C3-O-C12-trimethylsilylacetylene (ammonium) exhibits substantially longer t1/2 values than tenofovir in human liver microsomes, potent anti-HIV activity in vitro, and enhances pharmacokinetic properties in vivo. Tenofovir-C3-O-C12-trimethylsilylacetylene (ammonium) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

InhA-IN-7 (Compound 11) is a Triclocan (HY-B1119) derivative with inhibitory activity towards enoyl-acyl carrier protein reductase (InhA) with an IC₅₀ of 96 nM. InhA-IN-7 inhibits proliferations of Mycobacterium tuberculosis wildtype and mutant strains with MICs ranging from 19 to 75 μM.