Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor.
CPFX2090 is a cephalosporin antibacterial compound extracted from patent WO2013052568A1, Compound Example 16g[1].
Tetracycline hydrochloride is a broad-spectrum antibiotic used to treat a wide range of infections.
Gedivumab (MHAA4549A; RG7745) is a human monoclonal antibody that targets influenza A virus (IAV) with high specificity and binds to the highly conserved stem region of the IAV haemagglutinin protein, thereby preventing haemagglutinin maturation and blocking haemagglutinin-mediated membrane fusion in the intranucleosome. Gedivumab can be used in IAV infection disease studies[1].
Spiroxamine is a fungicide that can be used to kill grapes with less residue[1].
HLF1-11, a human lactoferrin-derived peptide, is a broad spectrum antimicrobial agent. HLF1-11 inhibits human MPO activity. HLF1-11 also directs GM-CSF-driven monocyte differentiation toward macrophages, and enhances immune responses[1][2].
Dicloxacillin sodium is a narrow-spectrum β-lactam antibiotic of the penicillin family. Dicloxacillin sodium is active against β-lactamase-producing organisms such as Staphylococcus aureus[1].
Grazoprevir hydrate (MK-5172 hydrate) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
Ravuconazole-d4 (BMS-207147-d4) is the deuterium labeled Ravuconazole. Ravuconazole (BMS-207147) is an orally available triazoleantifungle agent that potently inhibits a wide range of fungi[1][2].
SCYX-7158 is an effective, safe and orally active treatment for human african trypanosomiasis (HAT). In the T. b. brucei S427 strain, the MIC value for SCYX-7158 is 0.6 µg/mL.
Praziquantel is an anthelmintic effective against flatworms.Target: AntiparasiticPraziquantel is the drug of choice for treatment of all human schistosomes. Infected mice were treated with increasing Praziquantel doses until the highest dose of 3 × 300 mg/Kg was reached. The effect of Praziquantel treatment on the parasite population was assessed using five polymorphic microsatellite markers. Parasitological and genetic data were compared with those of the untreated control. After six parasite generations submitted to treatment, it was possible to obtain a S. mansoni population with decreased susceptibility to Praziquantel. In our experiments we also observed that female worms were more susceptible to Praziquantel than male worms [1, 2].
Flusilazole (DPX-H6573), an organosilane fungicide, has broad-spectrum antifungal effect. Flusilazole exhibits curative and preventative activities and is recommended for use in agriculture and horticulture[1].
Dolutegravir-d6 (S/GSK1349572-d6) is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2][3].
Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons.target: NS5A
3-O-cis-p-Coumaroyl maslinic acid (compound 16) is a natural compound isolated from the ethyl acetate extract of leaves of Miconia albicans.3-O-cis-p-Coumaroyl maslinic acid can inhibit PTP1B, with the IC50 of 0.46 μM, and shows antimicrobial activity on Gram-positive bacteria and yeasts[1][2].
MUT056399 is a highly potent inhibitor of the FabI enzyme of both S. aureus and E. coli with 50% inhibitory concentration IC50s of 12 nM and 58 nM, respectively. IC50 value: 12 nM (for S. aureus), 58 nM (for E. coli) [1]Target: FabI enzymein vitro: MUT056399 is a highly potent new inhibitor of the FabI enzyme of both Staphylococcus aureus and Escherichia coli. MUT056399 is very active against S. aureus strains, including methicillin-susceptible S. aureus (MSSA), methicillin-resistant S. aureus (MRSA), linezolid-resistant, and multidrug-resistant strains, with MIC90s between 0.03 and 0.12 μg/ml. MUT056399 is also active against coagulase-negative staphylococci, with MIC90s between 0.12 and 4 μg/ml. MUT056399 is very active against the 118 S. aureus strains tested, including MSSA and MRSA isolates and linezolid-resistant and multidrug-resistant strains, with MIC90s between ≤0.03 and 0.12 μg/ml.In vivo: MUT056399, administered subcutaneously, protected mice from a lethal systemic infection induced by MSSA, MRSA, and vancomycin-intermediate S. aureus strains (50% effective doses ranging from 19.3 mg/kg/day to 49.6 mg/kg/day). In the nonneutropenic murine thigh infection model, the same treatment with MUT056399 reduced the bacterial multiplication of MSSA and MRSA in the thighs of immunocompetent mice.
Abaecin is an antibacterial response peptide. Abaecin shows specific activity against an Apidaecin-resistant Xanthomonas strain[1].
Temporin C is an antimicrobial peptide against Legionella pneumophila[1].
Puromycin dihydrochloride is the dihydrochloride salt of puromycin. Puromycin is an aminoglycoside antibiotic that inhibits protein synthesis.
Atazanavir(BMS-232632) is an highly potent HIV-1 protease inhibitor.IC50 value:Target: HIV-1 protease inhibitorAtazanavir sulfate is a sulfate salt form of atazanavir that is an highly potent HIV-1 protease inhibitor. It has a pharmacokinetic profile that supports once-daily dosing and has demonstrated a unique resistance profile and superior virologic potency compared with other antiretrovirals in vitro. In subjects with HIV, atazanavir (400 mg once daily) produced rapid and sustained improvements in viral load and CD4 counts in both antiretroviral-naive as well as previously treated patients when used in combination with dual nucleoside reverse transcriptase inhibitor (NRTI) treatment [1].After intravenous (iv), oral (po) and intraportal (ip) administration of ATV at a dosage of 7 mg/kg, AUCs in HL rats were 12.41, 5.24 and 8.89 microg/mLh, respectively, and were significantly higher than those in control rats (4.09, 1.70 and 3.38 microg/mLh). Despite the decrease of distribution volume (Vd(ss)), the terminal half-life (t(1/2)) in HL tended to be shorter than in control, and hepatic distribution of ATV in HL rats was 4.8-fold increases. These results suggested that the uptake of ATV into liver might counteract the decrease of Vd(ss). On the other hand, there was no significant difference in bioavailability, and the lymphatic transport to AUC showed no statistical change. In conclusion, although the protein binding rate and AUC were significantly increased, the pharmacokinetics of ATV might be tolerated in HL [2].Clinical indications: HIV-1 infection Toxicity: torsades de pointes
Pyribencarb is a benzylcarbamate-type fungicide, which is active against a wide range of plant pathogenic fungi. Pyribencarb is a potent Qo inhibitor of cytochrome b. Pyribencarb is especially active against Botrytis cinerea and Sclerotinia sclerotirum[1].
Cefadroxil is a broad-spectrum antibiotic of the cephalosporin type, effective in Gram-positive and Gram-negative bacterial infections.
Isodiospyrin, a natural dimeric naphthoquinone, is a human DNA topoisomerase I (Topoisomerase) inhibitor. Isodiospyrin can prevent both DNA relaxation and kinase activities of human topoisomerase I. Isodiospyrin shows anticancer, antibacterial and antifungal activities[1][2][3].
D-Gluconic acid calcium hydrate is the carboxylic acid by the oxidation with antiseptic and chelating properties.
Indinavir(MK-639; L735524) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.Target: HIV ProteaseIndinavir(MK-639) is a protease inhibitor used as a component of highly active antiretroviral therapy (HAART) to treat HIV infection and AIDS.MK-639 appears to have significant dose-related antiviral activity and is well tolerated [1]. Inhibition constants (K(i)) of the antiviral drug indinavir for the reaction catalyzed by the mutant enzymes were about threefold and 50-fold higher for PR(L24I) and PR(I50V), respectively, relative to PR and PR(G73S). The dimer dissociation constant (K(d)) was estimated to be approximately 20 nM for both PR(L24I) and PR(I50V), and below 5 nM for PR(G73S) and PR. Crystal structures of the mutants PR(L24I), PR(I50V) and PR(G73S) were determined in complexes with indinavir, or the p2/NC substrate analog at resolutions of 1.10-1.50 Angstrom [2].
Amenamevir is a helicase-primase inhibitor which has potent antiviral activity against HSVs with an EC50 of 14 ng/mL.
AN2718 inhibits fungal growth by blocking protein synthesis using the oxaborole tRNA trapping (OBORT) mechanism.
Flutimide is a novel endonuclease inhibitor of influenza virus. Flutimide selectively inhibits endonuclease with an IC50 value of 3 μM. Flutimide shows antiviral activity in cell culture. Flutimide can be used for the research of acute contagious respiratory disease, such as influenza[1].
Dermaseptin, a peptide isolated from frog skin, exhibits potent antimicrobial activity against bacteria, fungi and protozoa.
Antituberculosis agent-8 (Compound 9i) is an antitubercular agent with an MIC of 3.53 μM (1.6 μg/mL) against M. tuberculosis H37Rv. Antituberculosis agent-8 also shows good antifungal activity against A. niger with an MIC of 62.50 μM[1].