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  • Title: Hepatitis C virus NS3 protease inhibitors comprising a novel aromatic P1 moiety.
    Author: Rönn R, Lampa A, Peterson SD, Gossas T, Akerblom E, Danielson UH, Karlén A, Sandström A.
    Journal: Bioorg Med Chem; 2008 Mar 15; 16(6):2955-67. PubMed ID: 18194867.
    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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