Structural highlights
Publication Abstract from PubMed
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.
P4 capped amides and lactams as HCV NS3 protease inhibitors with improved potency and DMPK profile.,Nair LG, Sannigrahi M, Bogen S, Pinto P, Chen KX, Prongay A, Tong X, Cheng KC, Girijavallabhan V, George Njoroge F Bioorg Med Chem Lett. 2010 Jan 15;20(2):567-70. Epub 2009 Nov 22. PMID:20004570[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Nair LG, Sannigrahi M, Bogen S, Pinto P, Chen KX, Prongay A, Tong X, Cheng KC, Girijavallabhan V, George Njoroge F. P4 capped amides and lactams as HCV NS3 protease inhibitors with improved potency and DMPK profile. Bioorg Med Chem Lett. 2010 Jan 15;20(2):567-70. Epub 2009 Nov 22. PMID:20004570 doi:10.1016/j.bmcl.2009.11.094
