Author/Authors :
Celia Dominguez، نويسنده , , Daniel E. Duffy، نويسنده , , Qi Han، نويسنده , , Richard S. Alexander، نويسنده , , Robert A. Galemmo Jr.، نويسنده , , Jeongsook M. Park، نويسنده , , Pancras C. Wong، نويسنده , , Eugene C. Amparo، نويسنده , , Robert M. Knabb، نويسنده , , Joseph Luettgen، نويسنده , , Ruth R. Wexler، نويسنده ,
Abstract :
Thrombin, a serine protease, phays a central role in the initiation of thrombotic events. We report the 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.
