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  • Title: Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
    Author: Bondada L, Rondla R, Pradere U, Liu P, Li C, Bobeck D, McBrayer T, Tharnish P, Courcambeck J, Halfon P, Whitaker T, Amblard F, Coats SJ, Schinazi RF.
    Journal: Bioorg Med Chem Lett; 2013 Dec 01; 23(23):6325-30. PubMed ID: 24135727.
    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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