Discovery of potent & selective inhibitors of activated thrombin-activatable fibrinolysis inhibitor for the treatment of thrombosis

ME Bunnage, J Blagg, J Steele, DR Owen…

Index: Bunnage, Mark E.; Blagg, Julian; Steele, John; Owen, Dafydd R.; Allerton, Charlotte; McElroy, Andrew B.; Miller, Duncan; Ringer, Tracy; Butcher, Ken; Beaumont, Kevin; Evans, Karen; Gray, Andrew J.; Holland, Stephen J.; Feeder, Neil; Moore, Robert S.; Brown, David G. Journal of Medicinal Chemistry, 2007 , vol. 50, # 24 p. 6095 - 6103

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Citation Number: 29

Abstract

Thrombin-activatable fibrinolysis inhibitor (TAFI) has emerged as a key link between the coagulation and fibrinolysis cascades and represents a promising new target for the treatment of thrombosis. A novel series of imidazolepropionic acids has been designed that exhibit high potency against activated TAFI (TAFIa) and excellent selectivity over plasma carboxypeptidase N (CPN). Structure activity relationships suggest that the imidazole ...