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

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

  • Bioorg Med Chem Lett. 2013 Dec 1;23(23):6325-30. doi: 10.1016/j.bmcl.2013.09.068.
Lavanya Bondada 1,  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
Affiliations

Affiliation

  • 1 Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Veterans Affairs Medical Center, 1670 Haygood Drive, NE, Atlanta, GA 30322, USA.
PMID: 24135727 DOI: 10.1016/j.bmcl.2013.09.068
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).

Keywords

Antiviral; HCV; Protease inhibitor.

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