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

Bioorganic & medicinal chemistry (2008-01-16)
Robert Rönn, Anna Lampa, Shane D Peterson, Thomas Gossas, Eva Akerblom, U Helena Danielson, Anders Karlén, Anja Sandström
RÉSUMÉ

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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Sigma-Aldrich
2-Aminobenzenesulfonamide, 98%
Sigma-Aldrich
2-Bromo-5-(trifluoromethyl)aniline, 97%