Hepatitis C NS5B polymerase inhibitors: 4,4-Dialkyl-1-hydroxy-3-oxo-3,4-dihydronaphthalene-3-yl benzothiadiazine derivatives

Douglas K. Hutchinson,Teresa Rosenberg,Larry L. Klein,Todd D. Bosse,Daniel P. Larson,Wenping He,Wen W. Jiang,Warren M. Kati,William E. Kohlbrenner,Yaya Liu,Sherie V. Masse,Tim Middleton,Akhteruzzaman Molla,Debra A. Montgomery,David W.A. Beno,Kent D. Stewart,Vincent S. Stoll,Dale J. Kempf

Bioorganic & Medicinal Chemistry Letters（2008）

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摘要

4,4-Dialkyl-1-hydroxy-3-oxo-3.4-dihydronaphthalene-3-yl benzothiadiazine derivatives were synthesized and evaluated as inhibitors of genotypes 1a and 1b HCV NS5B polymerase. A number of these compounds exhibited potent activity against genotypes 1a and 1b HCV polymerase in both enzymatic and cell culture activities. The representative compound above also showed favorable pharmacokinetics in the rat.

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关键词

Hepatitis C,HCV,HCV NS5B polymerase,Antiviral

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