1.
Bioorg Med Chem Lett
; 9(7): 925-30, 1999 Apr 05.
Artigo
em Inglês
| MEDLINE
| ID: mdl-10230612
RESUMO
Thrombin, a serine protease, plays 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.