European Journal of Medicinal Chemistry 2010-01-01

Hepatitis C virus NS3 protease inhibitors comprising a novel aromatic P1 moiety.

Miriam Carr, Lisa M. Greene, Andrew J.S. Knox, David G. Lloyd, Daniela M. Zisterer, Mary J. Meegan, Miriam Carr, Lisa M. Greene, Andrew J.S. Knox, David G. Lloyd, Daniela M. Zisterer, Mary J. Meegan, Miriam Carr, Lisa M. Greene, Andrew J.S. Knox, David G. Lloyd, Daniela M. Zisterer, Mary J. Meegan

Index: Bioorg. Med. Chem. 16(6) , 2955-67, (2008)

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Abstract

Inhibition of the hepatitis C virus (HCV) NS3 protease has emerged as an attractive approach to defeat the global hepatitis C epidemic. In this work, we present the synthesis and biochemical evaluation of HCV NS3 protease inhibitors comprising a non-natural aromatic P(1) moiety. A series of inhibitors with aminobenzoyl sulfonamides displaying submicromolar potencies in the full-length NS3 protease assay was prepared through a microwave-irradiated, palladium-catalyzed, amidocarbonylation protocol.