Tetrahydroquinoline Derivatives as Potent and Selective Factor XIa Inhibitors
Journal of Medicinal Chemistry2014Vol. 57(3), pp. 955–969
Citations Over TimeTop 10% of 2014 papers
Mimi L. Quan, Pancras C. Wong, Cailan Wang, Francis J. Woerner, Joanne M. Smallheer, Frank 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.
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