Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors
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- 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
- 关键词：HCV ; Protease inhibitor ; Antiviral
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：1 December, 2013
- 年：2013
- 卷：23
- 期：23
- 页码：6325-6330
- 全文大小：5805 K
文摘
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 渭M).