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Inhibitors of hepatitis C virus NS3.4A protease 1. Non-charged tetrapeptide variants |
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| 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 |
| Institution: | Vertex Pharmaceuticals Inc., 130 Waverly Street, Cambridge, MA 02139, USA. robert_perni@vrtx.com |
| Abstract: | 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 P1 and P2 inhibitor positions is discussed. |
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