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Hepatitis C virus NS3 protease inhibitors comprising a novel aromatic P1 moiety
Authors:Rönn Robert  Lampa Anna  Peterson Shane D  Gossas Thomas  Akerblom Eva  Danielson U Helena  Karlén Anders  Sandström Anja
Institution:Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry, Uppsala University, BMC, Box 574, SE-751 23 Uppsala, Sweden.
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.
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