The Design and Enzyme-Bound Crystal Structure of Indoline Based Peptidomimetic Inhibitors of Hepatitis C Virus NS3 Protease
Journal of Medicinal Chemistry2004Vol. 47(26), pp. 6443–6446
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Jesus M. Ontoria, Stefania Di Marco, Immacolata Conte, Maria Emilia Di Francesco, Cristina Gardelli, Uwe Koch, Victor G. Matassa, Marco Poma, Christian Steinkühler, Cinzia Volpari, Steven J. Harper
Abstract
The design of a series of peptidomimetic inhibitors of the hepatitis C virus NS3 protease is described. These inhibitors feature an indoline-2-carboxamide as a novel heterocyclic replacement for the P3 amino acid residue and N-terminal capping group of tripeptide based inhibitors. The crystal structure of the ternary NS3/NS4A/inhibitor complex for the most active molecule in this series highlights its suitability as an N-terminal capping group of a dipeptide inhibitor of the NS3 protease.
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