4.5 Article

P4 capped amides and lactams as HCV NS3 protease inhibitors with improved potency and DMPK profile

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 2, Pages 567-570

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.11.094

Keywords

HCV protease; Amides; Lactams

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SAR studies on the extension of P3 unit of Boceprevir (1, SCH 503034) with amides and lactams and their synthesis is described. Extensive SAR studies resulted in the identification of 36 bearing 4, 4-dimethyl lactam as the new P4 cap unit with improved potency (K-i* 15 nM, EC 90 = 70 nM) and pharmacokinetic properties (Rat AUC (PO) = 3.52 mu M h) compared to 1. (C) 2009 Elsevier Ltd. All rights reserved.

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