| Literature DB >> 24405333 |
Mimi L Quan1, Pancras C Wong, Cailan Wang, Francis Woerner, Joanne M Smallheer, Frank A Barbera, Jeffrey M Bozarth, Randi L Brown, Mark R Harpel, Joseph M Luettgen, Paul E Morin, Tara Peterson, Vidhyashankar Ramamurthy, Alan R Rendina, Karen A Rossi, Carol A Watson, Anzhi Wei, Ge Zhang, Dietmar Seiffert, Ruth R Wexler.
Abstract
Antithrombotic agents that are inhibitors of factor XIa (FXIa) have the potential to demonstrate robust efficacy with a low bleeding risk profile. Herein, we describe a series of tetrahydroquinoline (THQ) derivatives as FXIa inhibitors. Compound 1 was identified as a potent and selective tool compound for proof of concept studies. It exhibited excellent antithrombotic efficacy in rabbit thrombosis models and did not prolong bleeding times. This demonstrates proof of concept for the FXIa mechanism in animal models with a reversible, small molecule inhibitor.Entities:
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Year: 2014 PMID： 24405333 DOI： 10.1021/jm401670x
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446