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2. Inhibitors of hepatitis C virus NS3·4A protease 2. Warhead SAR and optimization

Author

Perni, Robert B., primary, Pitlik, Janos, additional, Britt, Shawn D., additional, Court, John J., additional, Courtney, Lawrence F., additional, Deininger, David D., additional, Farmer, Luc J., additional, Gates, Cynthia A., additional, Harbeson, Scott L., additional, Levin, Rhonda B., additional, Lin, Chao, additional, Lin, Kai, additional, Moon, Young-Choon, additional, Luong, Yu-Ping, additional, O'Malley, Ethan T., additional, Rao, B.Govinda, additional, Thomson, John A., additional, Tung, Roger D., additional, Van Drie, John H., additional, and Wei, Yunyi, additional

Published
2004
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3. Inhibitors of hepatitis C virus NS3·4A protease 1. Non-Charged tetrapeptide variants

Author

Perni, Robert B., primary, Britt, Shawn D., additional, Court, John C., additional, Courtney, Lawrence F., additional, Deininger, David D., additional, Farmer, Luc J., additional, Gates, Cynthia A., additional, Harbeson, Scott L., additional, Kim, Joseph L., additional, Landro, James A., additional, Levin, Rhonda B., additional, Luong, Yu-Ping, additional, O'Malley, Ethan T., additional, Pitlik, Janos, additional, Rao, B.Govinda, additional, Schairer, Wayne C., additional, Thomson, John A., additional, Tung, Roger D., additional, Van Drie, John H., additional, and Wei, Yunyi, additional

Published
2003
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4. Inhibitors of Hepatitis C Virus NS3.4A Protease: P2 Proline Variants

Author

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

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.

Published
2005

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