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

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

Volume: 2 Issue: 7

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

Affiliation:

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

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.

Cite this article as:

Luong P. Yu-, Perni B. Robert, Wei Yunyi, Van Drie H. John, Tung D. Roger, Thomson A. John, Schairer C. Wayne, Rao G. B., Pitlik Janos, Maxwell P. John, Farmer J. Luc, Lin Chao, Lin Kai, Harbeson L. Scott, Gates A. Cynthia, Deininger D. David, Courtney F. Lawrence, Court J. John, Cottrell M. Kevin and Britt D. Shawn, Inhibitors of Hepatitis C Virus NS3.4A Protease: P2 Proline Variants, Letters in Drug Design & Discovery 2005; 2 (7) . https://dx.doi.org/10.2174/157018005774479203