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Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors |
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| Authors: | Lavanya Bondada Ramu Rondla Ugo Pradere Peng Liu Chengwei Li Drew Bobeck Tamara McBrayer Philip Tharnish Jerome Courcambeck Philippe Halfon Tony Whitaker Franck Amblard Steven J. Coats Raymond F. Schinazi |
| Affiliation: | 1. Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Veterans Affairs Medical Center, 1670 Haygood Drive, NE, Atlanta, GA 30322, USA;2. RFS Pharma, LLC, 1860 Montreal Road, Tucker, GA 30084, USA;3. Genoscience-Pharma, 10 rue d’Iena, 13006 Marseille, France |
| Abstract: | Herein, we report the synthesis and structure–activity relationship studies of new analogs of boceprevir 1 and telaprevir 2. Introduction of azetidine and spiroazetidines as a P2 substituent that replaced the pyrrolidine moiety of 1 and 2 led to the discovery of a potent hepatitis C protease inhibitor 37c (EC50 = 0.8 μM). |
| Keywords: | HCV Protease inhibitor Antiviral |
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