Bioorganic and Medicinal Chemistry Letters p. 925 - 930 (1999)
Update date:2022-08-03
Topics:
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.
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.
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