Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors
作者: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
DOI:10.1016/j.bmcl.2013.09.068
日期:2013.12
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 mu M). (C) 2013 Elsevier Ltd. All rights reserved.