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Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.

Authors :
Bondada, Lavanya
Rondla, Ramu
Pradere, Ugo
Liu, Peng
Li, Chengwei
Bobeck, Drew
McBrayer, Tamara
Tharnish, Philip
Courcambeck, Jerome
Halfon, Philippe
Whitaker, Tony
Amblard, Franck
Coats, Steven J.
Schinazi, Raymond F.
Source :
Bioorganic & Medicinal Chemistry Letters. Dec2013, Vol. 23 Issue 23, p6325-6330. 6p.
Publication Year :
2013

Abstract

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 =0.8μM). [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
23
Issue :
23
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
91725759
Full Text :
https://doi.org/10.1016/j.bmcl.2013.09.068