| Literature DB >> 23927973 |
Scott A Bolton1, James C Sutton, Rushith Anumula, Gregory S Bisacchi, Bruce Jacobson, William A Slusarchyk, Uwe D Treuner, Shung C Wu, Guohua Zhao, Zulan Pi, Steven Sheriff, Rebecca A Smirk, Sharon Bisaha, Daniel L Cheney, Anzhi Wei, William A Schumacher, Karen S Hartl, Eddie Liu, Robert Zahler, Steven M Seiler.
Abstract
In this Letter, we describe the synthesis of several nonamidine analogs of biaryl acid factor VIIa inhibitor 1 containing weakly basic or nonbasic P1 groups. 2-Aminoisoquinoline was found to be an excellent surrogate for the benzamidine group (compound 2) wherein potent inhibition of factor VIIa is maintained relative to most other related serine proteases. In an unanticipated result, the m-benzamide P1 (compounds 21a and 21b) proved to be a viable benzamidine replacement, albeit with a 20-40 fold loss in potency against factor VIIa.Entities:
Keywords: 2-Aminoisoquinoline; Factor VIIa; Inhibition
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Year: 2013 PMID： 23927973 DOI： 10.1016/j.bmcl.2013.06.028
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823