Toxicologie

Applications Morphazinamide is an anti-tuberculosis agent. Also, it is derived from Pyrazinamide (P840600), which is an anti-bacterial (tuberculostatic).
References Gennaro, M. C., et al.: J. Chromatogr. B Biomed. Sci. Appl., 754, 477-486 (2001); Weiner, I.M., et al.: J. Pharmacol. Exp. Ther., 180, 411 (1972), Feldner, E., et al.: Anal. Profiles Drug Subs., 12, 433 (1983)

Applications 4-​[3-Fluoro-​4-​(methoxycarbonyl)​phenyl]​-​1,​1-​dimethylethyl Ester 1-​Piperazinecarboxylic Acid is used in the binding envelope of cytochrome P 450 51 inhibitors targeting Trypanosoma cruzi with 4-aminopyridyl-based sulfonamide derivatives.
References Vieira, Debora F. et al., ChemBioChem. 8,1111-1120(2014);

Applications 3,4-Dihydroquinoline-2-one 6-Oxoacetic Acid is a derivative of 3,4-Dihydro-2-quinolone (D450600), which is used to prepare potent bicyclic peptide deformylase inhibitors with antibacterial effects. It is also used to synthetisze substituted iminopiperidines as inhibitors of human nitric oxide synthase isoforms.
References Molteni, V., et al.: Bioorg. Med. Chem. lett., 14, 1477 (2004); Webber, R., et al.: J. Med. Chem., 41, 96 (1998)

Applications N-Benzoyl-2'-deoxy-2',2'-difluorocytidine 3’-Benzoate is an intermediate in the synthesis of Gemcitabine (G305000) metabolites.
References Baraniak, J., et al.: Bioorg. Med. Chem., 22, 2133 (2014); Labrioli, M.A., et al.: Bioorg. Med. Chem., 22, 2303 (2014);

Applications ((((R)-1-(6-((((5-Fluoro-1-((2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl)-2-oxo-1,2-dihydropyrimidin-4-yl)amino)methyl)amino)-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphonic acid is impurity of Emtricitabine (E525000), a reverse transcriptase inhibitor. It is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner. A nucleoside analog structurally related to Lamivudine (L172500).
References FASEB J., 13, 1511 (1999), Molina, J.-M., et al.: J. InfecSchinazi, R.F., et al.: Antimicrob. Ag. Chemother., 36, 2423 (1992), Shockeor, J.P., et al.: Xenobioica, 26, 189 (1996), Feng, J.Y., et al.: . Dis., 182, 599 (2000)

Applications Verazide is derived from Isoniazid (I821450), which is an antibiotic for treatment of Mycobacterium tuberculosis, inhibits mycolic acid biosynthesis. Metabolized by hepatic N-acetyltransferase (NAT) and cytochrome P450 2E1 (CYP2E1) to form hepatotoxins. Selectively induces expression of CYP2E1. Reversibly inhibits CYP2C19 and CYP3A4 activities, and mechanistically inactivates CYP1A2, CYP2A6, CYP2C19 and CYP3A4 at clinically relevant concentrations. Antibacterial (tuberculostatic).
References Brewer, G.A., et al.: Anal. Profiles Drug Subs., 6, 183 (1977), Weber, W.W., et al.: Clin. Pharmacokinet., 4, 401 (1979)

Applications 2-(1-Ethylpropyl)-2,4-dihydro-4-[4-[4-(4-methoxyphenyl)-1-piperazinyl]phenyl]-3H-1,2,4-triazol-3-one is an intermediate in the synthesis of Deshydroxy Posaconazole Impurity (A6480252), which is a 2,2,5-tetrahydrofuran regioisomers of SCH 51048 (A648025) that exhibit antifungal activity.
References Lovey, R.G.; et al.: Bioorganic Med. Chem. Lett, 12, 1739 (2002)

Applications Isodecyl Daptomycin is an impurity of Daptomycin (D193350), a cyclic lipopeptide antibiotic derived from a fermentation product of Streptomyces roseosporus. Daptomycin disrupts plasma membrane function in gram-positive bacteria.
References Allen, N.E., et al.: Antimicrob. Agents Chemother., 31, 1093 (1987);Tully, F.P., et al.: Expert Opin. Invest. Drugs, 8, 1223 (1999)