Tenofovir amibufenamide (HS-10234), a Tenofovir prodrug, is an orally active antiviral agent. Tenofovir amibufenamide inhibits HBV, and can be used for chronic hepatitis B (CHB) study[1][2].
Megazol is an orally active antibacterial agent. Megazol has effective inhibitory against T. b. brueei with an EC50 of 0.01 μg/mL. Megazol can be used for the research of protozoan infections[1].
Antibacterial agent 100 (Compound 7c) is an antibacterial and antifungal agent. Antibacterial agent 100 shows promising activity with MIC values of 4, 4 and 8 μg/mL against Staphylococcus aureus, Candida albicans and Cryptococcus neoformans, respectively[1].
Trimetrexate trihydrochloride is a antibiotic, also a potent dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate trihydrochloride can be used for researching Pneumocystis carinii pneumonia (PCP)[1][2].
Norvancomycin hydrochloride is applicable for endocarditis, osteomyelitis, pneumonia, sepsis or soft tissue infections causedby Staphylococcus (including Methicillin-resistant strains and multidrug-resistant microbial strains).Target: Antibacterial
9-Carboxymethoxymethylguanine is the main metabolite of Aciclovir. Acyclovir (Aciclovir) is a guanosine analogue and an orally active antiviral agent[1].
Antibacterial agent 105 (Compound 17) is a phenanthrolinic analog of quinolones show antibacterial activity against M. tuberculosis with antibacterial activity (MIC90=2.64 μM)。Antibacterial agent 105 exhibits antibacterial activities against different bacterial species with MIC90s of 11.18, 11.18，0.70，1.40，44.70, and 22.35 μM for M. smegmatis, M. aurum, M. marinum,BCG, E. aerogenes and S. aureus, respectively[1].
Flutriafol is a triazole fungicide with broad spectrum fungicidal activity.
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: AntibioticEperezolid 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].
Kanamycin (Kanamycin A) is an orally active antibacterial (gram-negative/positive bacteria) agent, inhibits translocation and causes misencoding by binding to the 70 S ribosomal subunit. Kanamycin shows good inhibitory activity to both M. tuberculosis (sensitive and drug-resistant ) and K. pneumonia, which can be used in studies of tuberculosis and pneumonia[1][2][3][4].
Borrelidin (Treponemycin) is a nitrile-containing macrolide antibiotic isolated from Streptomyces rochei, which acts as an inhibitor of bacterial and eukaryal threonyl-tRNA synthetase, can target ALL cell lines by inducing apoptosis and mediating G(1) arrest. Borrelidin (Treponemycin) is an inhibitor of a cyclin-dependent kinase (CDK) of the budding yeast, Cdc28/Cln2 with an IC50 of 24 μM. Borrelidin (Treponemycin) is a potent angiogenesis inhibitor with an IC50 of 0.8 nM for capillary tube formation, and induces apoptosis of the tube-forming cells. Borrelidin (Treponemycin) has strong antimalarial activities, with IC50s of 1.9 nM and 1.8 nM against K1 and FCR3 strains of Plasmodium falciparum[1][2][3].
HIV-1 inhibitor-16 (compound 7a) is a highly potent HIV-1 inhibitor with an EC50 value of 1.3 nM for HIV-1 WT. HIV-1 inhibitor-16 also has certain inhibitory activity against HIV-1 K103N, E138K, Y181C and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM and 35 nM. HIV-1 inhibitor-16 has favorable solubility and liver microsome stability, and does not exhibit apparent CYP enzymatic inhibitory activity or acute toxicity[1].
Garenoxacin mesylate hydrate is a novel oral des-fluoro(6) quinolone with potent antimicrobial activity, against common respiratory pathogens, including resistant strains.
Pristinamycin IIA (RP 12536) is a macrocyclic lactone peptolide antibiotic, derived from Streptomyces pristinaespiralis, which is a member of the streptogramin A group of antibiotics[1].
Bischloroanthrabenzoxocinone is a potent Type II fatty acid synthesis (FASII) inhibitor. Bischloroanthrabenzoxocinone inhibits fatty acid synthesis. Bischloroanthrabenzoxocinone shows antibacterial activities and inhibits phospholipid, DNA, RNA, protein, and cell wall synthesis[1].
QPX7728-OH disodium (compound 13) is a boronic acid β-lactamase inhibitor, exacted from WO2018005662A1, compound 13. QPX7728-OH disodium inhibits cleavage of Nitrocefin (HY-108913) by purified class A, C and D enzymes, with Kis less than 0.1 µΜ[1].
HBV-IN-20 is a potent and oral active HBV inhibitor with an EC50 of 0.46 µM. HBV-IN-20 is a typical type II CpAM (core protein assembly modulators)[1].
Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2[1][2][3][4][5][6].
Influenza virus-IN-4 (compound 11e) is a potent influenza virus neuraminidase inhibitor with IC50s of 3.4, 0.094, 0.79, 0.077 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-4 shows NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-4 shows low cytotoxicity with an CC50 of >200 µM. Influenza virus-IN-4 shows no obvious toxicity at the dose of 1500 mg/kg in mice[1].
SARS-CoV-2-IN-16 (Compound 12) is a potent SARS-CoV-2 nucleocapsid protein (NPro) inhibitor. SARS-CoV-2-IN-16 exhibits potent anti-viral activity with the EC50 of 3.69 μM. SARS-CoV-2-IN-16 binds to NPro with the low KD value of 7.82 μM, suggesting that SARS-CoV-2-IN-16 is a potent NPro ligand[1].
Fluazinam is a broad spectrum pyridinamine fungal inhibitor.
Difloxacin is an antimicrobial agent[1].
GSK2838232 inhibit HIV reverse transcriptase activity across a broad panel of HIV-1 isolates, extracted from patent WO/2013090664A1, compound51.
Anisofolin A is a flavonoid that can be isolated from Anisomeles indica. Anisofolin A has antimalarial activity (IC50: 4.39 μM), and antimycobacterium activity (IC50: 4.50 μM) against M. tuberculosis H37Ra[1].
IMB-301 is a HIV-1 auxilins Vif degradation hA3G antagonist. IMB-301 inhibits hA3G-Vif interactions to inhibit Vif degradations hA3G. IMB-301 has anti-HIV-1 activity[1].
A mixture of uvaretin and isouvaretin (HY-N10130) exhibits significant antibacterial activity against B. subtilis (EC50 8.7 μM) and S. epidermidis (IC50 7.9 μM).
PqsR/LasR-IN-3 (Compound 7a) is a potent inhibitor of PqsR and LasR systems in P. aeruginosa. PqsR/LasR-IN-3 also inhibits hERG with the IC50 of 109.01 µM[1].
Curcumin D6 (Diferuloylmethane D6) is a deuterium labeled Curcumin (Turmeric yellow). Curcumin (Turmeric yellow) is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase (HATs) and also shows inhibitory effects on NF-κB and MAPKs.
CDK9-IN-30 is a CDK9 inhibitor that inhibits HIV-1 viral replication[1].
Filastatin is a long-lasting inhibitor of Candida albicans filamentation. Filastatin inhibits adhesion by multiple pathogenic Candida species with an IC50 of ~3 μM in the GFP-based adhesion assay. Filastatin inhibits fungal adhesion to polystyrene and human cells, the yeast-to-hyphal morphological transition, induction of the hyphal-specific HWP1 promoter. Filastatin has potent antifungal effect[1].