| Literature DB >> 19054673 |
Frank Ruebsam1, Chinh V Tran, Lian-Sheng Li, Sun Hee Kim, Alan X Xiang, Yuefen Zhou, Julie K Blazel, Zhongxiang Sun, Peter S Dragovich, Jingjing Zhao, Helen M McGuire, Douglas E Murphy, Martin T Tran, Nebojsa Stankovic, David A Ellis, Alberto Gobbi, Richard E Showalter, Stephen E Webber, Amit M Shah, Mei Tsan, Rupal A Patel, Laurie A Lebrun, Huiying J Hou, Ruhi Kamran, Maria V Sergeeva, Darian M Bartkowski, Thomas G Nolan, Daniel A Norris, Leo Kirkovsky.
Abstract
5,6-Dihydro-1H-pyridin-2-one analogs were discovered as a novel class of inhibitors of genotype 1 HCV NS5B polymerase. Among these, compound 4ad displayed potent inhibitory activities in biochemical and replicon assays (IC(50) (1b)<10nM; IC(50) (1a)<25nM, EC(50) (1b)=16nM), good in vitro DMPK properties, as well as moderate oral bioavailability in monkeys (F=24%).Entities:
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Year: 2008 PMID： 19054673 DOI： 10.1016/j.bmcl.2008.11.048
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823