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. 2010 Jan 15;20(2):567-70.
doi: 10.1016/j.bmcl.2009.11.094. Epub 2009 Nov 22.

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

Latha G Nair  1 , Mousumi Sannigrahi, Stephane Bogen, Patrick Pinto, Kevin X Chen, Andrew Prongay, Xiao Tong, K-C Cheng, Viyyoor Girijavallabhan, F George Njoroge
Affiliations

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

Latha G Nair et al. Bioorg Med Chem Lett. .

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.

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