| Literature DB >> 20004570 |
Latha G Nair1, Mousumi Sannigrahi, Stephane Bogen, Patrick Pinto, Kevin X Chen, Andrew Prongay, Xiao Tong, K-C Cheng, Viyyoor Girijavallabhan, F George Njoroge.
Abstract
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)( *)=15nM, EC 90=70nM) and pharmacokinetic properties (Rat AUC (PO)=3.52microMh) compared to 1. Copyright 2009 Elsevier Ltd. All rights reserved.Entities:
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Year: 2009 PMID： 20004570 DOI： 10.1016/j.bmcl.2009.11.094
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823