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.
|Original language||English (US)|
|Number of pages||4|
|Journal||Journal of medicinal chemistry|
|State||Published - Dec 4 2003|
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery