Development of carboxylic acid replacements in indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase

I Stansfield, M Pompei, I Conte, C Ercolani…

Index: Stansfield, Ian; Pompei, Marco; Conte, Immacolata; Ercolani, Caterina; Migliaccio, Giovanni; Jairaj, Mark; Giuliano, Claudio; Rowley, Michael; Narjes, Frank Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 18 p. 5143 - 5149

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Citation Number: 27

Abstract

Allosteric inhibition of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase enzyme has recently emerged as a viable strategy toward blocking replication of viral RNA in cell-based systems. We report here 2 series of indole-N-acetamides, bearing physicochemically diverse carboxylic acid replacements, which show potent affinity for the NS5B enzyme with reduced potential for formation of glucuronide conjugates. Preliminary ...