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

Bioorganic & Medicinal Chemistry Letters
2013.0

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).

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