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

…, D Colussi, M Bosserman, C Burlein…

文献索引：Barrow, James C.; Nantermet, Philippe G.; Stauffer, Shaun R.; Ngo, Phung L.; Steinbeiser, Melissa A.; Mao, Shi-Shan; Carroll, Steven S.; Bailey, Carolyn; Colussi, Dennis; Bosserman, Michelle; Burlein, Christine; Cook, Jacquelynn J.; Sitko, Gary; Tiller, Philip R.; Miller-Stein, Cynthia M.; Rose, Mark; McMasters, Daniel R.; Vacca, Joseph P.; Selnick, Harold G. Journal of Medicinal Chemistry, 2003 , vol. 46, # 25 p. 5294 - 5297

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被引用次数: 34

摘要

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 ...