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Ruebsam, Frank; Tran, Chinh V; Li, Lian-Sheng; Kim, Sun Hee; Xiang, Alan X; Zhou, Yuefen; Blazel, Julie K; Sun, Zhongxiang; Dragovich, Peter S; Zhao, Jingjing; McGuire, Helen M; Murphy, Douglas E; Tran, Martin T; Stankovic, Nebojsa; Ellis, David A; Gobbi, Alberto; Showalter, Richard E; Webber, Stephen E; Shah, Amit M; Tsan, Mei; Patel, Rupal A; Lebrun, Laurie A; Hou, Huiying J; Kamran, Ruhi; Sergeeva, Maria V; Bartkowski, Darian M; Nolan, Thomas G; Norris, Daniel A; Kirkovsky, Leo
Bioorganic & medicinal chemistry letters, 01/2009, Letnik: 19, Številka: 2Journal Article
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%).
