228552-26-9Relevant articles and documents
Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors
Dominguez, Celia,Duffy, Daniel E.,Han, Qi,Alexander, Richard S.,Galemmo Jr., Robert A.,Park, Jeongsook M.,Wong, Pancras C.,Amparo, Eugene C.,Knabb, Robert M.,Luettgen, Joseph,Wexler, Ruth R.
, p. 925 - 930 (1999)
Thrombin, a serine protease, plays a central role in the initiation of thrombotic events. We report design, synthesis, and antithrombotic efficacy of XU817 (7), a nonpeptide 5-(amidino) indole thrombin inhibitor. Utilizing the co-crystal structure of XU817 bound in the active site of thrombin we were able to synthesize analogs with enhanced thrombin affinity.
