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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Inhibitors of Hepatitis C Virus NS3.4A Protease: P2 Proline Variants

Author(s): Yu- P. Luong, Robert B. Perni, Yunyi Wei, John H. Van Drie, Roger D. Tung, John A. Thomson, Wayne C. Schairer, B. G. Rao, Janos Pitlik, John P. Maxwell, Luc J. Farmer, Chao Lin, Kai Lin, Scott L. Harbeson, Cynthia A. Gates, David D. Deininger, Lawrence F. Courtney, John J. Court, Kevin M. Cottrell and Shawn D. Britt

Volume 2, Issue 7, 2005

Page: [497 - 502] Pages: 6

DOI: 10.2174/157018005774479203

Price: $65

Abstract

A series of novel bicyclic proline P2 scaffold based tetrapeptide inhibitors were designed and prepared. Given their relatively small size, these compounds exhibited exceptional binding affinities and good cellular potencies for HCV protease. One of the best analogues, tricyclic based P2 scaffold 12, had an affinity for HCV with a Ki of 37 nM and cell activity IC50 of 200 nM.

Keywords: Hepatitis C, NS3, , 4A protease, tetrapeptide inhibitors, VX-950, bicyclic proline, P2 scaffolds

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