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. 2003 Dec 4;46(25):5294-7.
doi: 10.1021/jm034141y.

Synthesis and evaluation of imidazole acetic acid inhibitors of activated thrombin-activatable fibrinolysis inhibitor as novel antithrombotics

James C Barrow  1 , Philippe G Nantermet, Shaun R Stauffer, Phung L Ngo, Melissa A Steinbeiser, Shi-Shan Mao, Steven S Carroll, Carolyn Bailey, Dennis Colussi, Michelle Bosserman, Christine Burlein, Jacquelynn J Cook, Gary Sitko, Philip R Tiller, Cynthia M Miller-Stein, Mark Rose, Daniel R McMasters, Joseph P Vacca, Harold G Selnick
Affiliations

Synthesis and evaluation of imidazole acetic acid inhibitors of activated thrombin-activatable fibrinolysis inhibitor as novel antithrombotics

James C Barrow et al. J Med Chem. .

Abstract

Thrombin-activatable fibrinolysis inhibitor (TAFI) is an important regulator of fibrinolysis, and inhibitors of this enzyme have potential use in antithrombotic and thrombolytic therapy. Appropriately substituted imidazole acetic acids such as 10j were found to be potent inhibitors of activated TAFI and selective versus the related carboxypeptidases CPA, CPN, and CPM but not CPB. Further, 10j accelerated clot lysis in vitro and was shown to be efficacious in a primate model of thrombosis.

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