| Literature DB >> 16697194 |
Nigel S Watson1, David Brown, Matthew Campbell, Chuen Chan, Laiq Chaudry, Máire A Convery, Rebecca Fenwick, J Nicole Hamblin, Claudine Haslam, Henry A Kelly, N Paul King, Cynthia L Kurtis, Andrew R Leach, Gary R Manchee, Andrew M Mason, Charlotte Mitchell, Champa Patel, Vipulkumar K Patel, Stefan Senger, Gita P Shah, Helen E Weston, Caroline Whitworth, Robert J Young.
Abstract
A series of novel, non-basic 3-(6-chloronaphth-2-ylsulfonyl)aminopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating an alanylamide P4 group, was designed and synthesised. Within this series, the N-2-(morpholin-4-yl)-2-oxoethyl derivative 24 was shown to be a potent, selective fXa inhibitor with good anticoagulant activity. Moreover, 24 possessed highly encouraging rat and dog pharmacokinetic profiles with excellent oral bioavailabilities in both species.Entities:
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Year: 2006 PMID： 16697194 DOI： 10.1016/j.bmcl.2006.04.053
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823