| Literature DB >> 20121197 |
Shouming Wang1, Richard Beck, Andrew Burd, Toby Blench, Frederic Marlin, Tenagne Ayele, Stuart Buxton, Claudio Dagostin, Maja Malic, Rina Joshi, John Barry, Mohammed Sajad, Chiming Cheung, Shaheda Shaikh, Suresh Chahwala, Chaman Chander, Christine Baumgartner, Hans-Peter Holthoff, Elizabeth Murray, Michael Blackney, Amanda Giddings.
Abstract
On the basis of our understanding on the binding interactions of the benzothiophene template within the FIXa active site by X-ray crystallography and molecular modeling studies, we developed our SAR strategy by targeting the 4-position of the template to access the S1 beta and S2-S4 sites. A number of highly selective and potent factor Xa (FXa) and FIXa inhibitors were identified by simple switch of functional groups with conformational changes toward the S2-S4 sites.Entities:
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Year: 2010 PMID： 20121197 DOI： 10.1021/jm901476x
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446