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Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition.
Wu YJ, Davis CD, Dworetzky S, Fitzpatrick WC, Harden D, He H, Knox RJ, Newton AE, Philip T, Polson C, Sivarao DV, Sun LQ, Tertyshnikova S, Weaver D, Yeola S, Zoeckler M, Sinz MW. Wu YJ, et al. Among authors: yeola s. J Med Chem. 2003 Aug 28;46(18):3778-81. doi: 10.1021/jm034111v. J Med Chem. 2003. PMID: 12930139
Discovery of (S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S,Z)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide (BMS-433796): a gamma-secretase inhibitor with Abeta lowering activity in a transgenic mouse model of Alzheimer's disease.
Prasad CV, Zheng M, Vig S, Bergstrom C, Smith DW, Gao Q, Yeola S, Polson CT, Corsa JA, Guss VL, Loo A, Wang J, Sleczka BG, Dangler C, Robertson BJ, Hendrick JP, Roberts SB, Barten DM. Prasad CV, et al. Among authors: yeola s. Bioorg Med Chem Lett. 2007 Jul 15;17(14):4006-11. doi: 10.1016/j.bmcl.2007.04.082. Epub 2007 Apr 30. Bioorg Med Chem Lett. 2007. PMID: 17502137
Inhibitors of HIV-1 attachment. Part 2: An initial survey of indole substitution patterns.
Meanwell NA, Wallace OB, Fang H, Wang H, Deshpande M, Wang T, Yin Z, Zhang Z, Pearce BC, James J, Yeung KS, Qiu Z, Kim Wright JJ, Yang Z, Zadjura L, Tweedie DL, Yeola S, Zhao F, Ranadive S, Robinson BA, Gong YF, Wang HG, Spicer TP, Blair WS, Shi PY, Colonno RJ, Lin PF. Meanwell NA, et al. Among authors: yeola s. Bioorg Med Chem Lett. 2009 Apr 1;19(7):1977-81. doi: 10.1016/j.bmcl.2009.02.040. Epub 2009 Feb 13. Bioorg Med Chem Lett. 2009. PMID: 19251416
Aminotriazine 5-HT7 antagonists.
Mattson RJ, Denhart DJ, Catt JD, Dee MF, Deskus JA, Ditta JL, Epperson J, Dalton King H, Gao A, Poss MA, Purandare A, Tortolani D, Zhao Y, Yang H, Yeola S, Palmer J, Torrente J, Stark A, Johnson G. Mattson RJ, et al. Among authors: yeola s. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4245-8. doi: 10.1016/j.bmcl.2004.06.008. Bioorg Med Chem Lett. 2004. PMID: 15261279
Comparative metabolism of radiolabeled muraglitazar in animals and humans by quantitative and qualitative metabolite profiling.
Zhang D, Wang L, Raghavan N, Zhang H, Li W, Cheng PT, Yao M, Zhang L, Zhu M, Bonacorsi S, Yeola S, Mitroka J, Hariharan N, Hosagrahara V, Chandrasena G, Shyu WC, Humphreys WG. Zhang D, et al. Among authors: yeola s. Drug Metab Dispos. 2007 Jan;35(1):150-67. doi: 10.1124/dmd.106.012450. Epub 2006 Oct 24. Drug Metab Dispos. 2007. PMID: 17062777 Clinical Trial.
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