Article
Structure-based design, synthesis, and biological evaluation of 1,1-dioxoisothiazole and benzo[b]thiophene-1,1-dioxide derivatives as novel inhibitors of hepatitis C virus NS5B polymerase.
Bioorganic & medicinal chemistry letters - 15 Jul 2008
Kim Sun Hee, Tran Martin T, Ruebsam Frank, Xiang Alan X, Ayida Benjamin, McGuire Helen, Ellis David, Blazel Julie, Tran Chinh V, Murphy Douglas E, Webber Stephen E, Zhou Yuefen, Shah Amit M, Tsan Mei, Showalter Richard E, Patel Rupal, Gobbi Alberto, LeBrun Laurie A, Bartkowski Darian M, Nolan Thomas G, Norris Daniel A, Sergeeva Maria V, Kirkovsky Leo, Zhao Qiang, Han Qing, Kissinger Charles R
Abstract excerpt
A novel series of HCV NS5B polymerase inhibitors comprising 1,1-dioxoisothiazoles and benzo[b]thiophene-1,1-dioxides were designed, synthesized, and evaluated. SAR studies guided by structure-based design led to the identification of a number of potent NS5B inhibitors with nanomolar IC(50) values. The most potent compound exhibited IC(50) less than 10nM against the genotype 1b HCV polymerase and EC(50) of 70 nM...
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