These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: P4 capped amides and lactams as HCV NS3 protease inhibitors with improved potency and DMPK profile.
    Author: Nair LG, Sannigrahi M, Bogen S, Pinto P, Chen KX, Prongay A, Tong X, Cheng KC, Girijavallabhan V, George Njoroge F.
    Journal: Bioorg Med Chem Lett; 2010 Jan 15; 20(2):567-70. PubMed ID: 20004570.
    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.
    [Abstract] [Full Text] [Related] [New Search]