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

Tetrapeptide-based peptidomimetic compounds have been shown to effectively inhibit the hepatitis C virus NS3·4A protease without the need of a charged functionality. An aldehyde is used as a prototype reversible electrophilic warhead. The SAR of the P 1 and P 2 inhibitor positions is discussed. The...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2003-11, Vol.13 (22), p.4059-4063
Main Authors: Perni, Robert B., Britt, Shawn D., Court, John C., Courtney, Lawrence F., Deininger, David D., Farmer, Luc J., Gates, Cynthia A., Harbeson, Scott L., Kim, Joseph L., Landro, James A., Levin, Rhonda B., Luong, Yu-Ping, O'Malley, Ethan T., Pitlik, Janos, Rao, B.Govinda, Schairer, Wayne C., Thomson, John A., Tung, Roger D., Van Drie, John H., Wei, Yunyi
Format: Article
Language:English
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Summary:Tetrapeptide-based peptidomimetic compounds have been shown to effectively inhibit the hepatitis C virus NS3·4A protease without the need of a charged functionality. An aldehyde is used as a prototype reversible electrophilic warhead. The SAR of the P 1 and P 2 inhibitor positions is discussed. The synthesis and structure–activity relationships of a novel series of reversible covalent inhibitors of the hepatitis C NS3·4A protease are described.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2003.08.050