| Literature DB >> 24135727 |
Lavanya Bondada1, 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.
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).Entities:
Keywords: Antiviral; HCV; Protease inhibitor
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Year: 2013 PMID： 24135727 PMCID： PMC4042666 DOI： 10.1016/j.bmcl.2013.09.068
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823