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Bioorg Med Chem Lett. 1999 Apr 5;9(7):925-30.

Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors.

Author information

1
DuPont Pharmaceuticals Company, Wilmington, DE 19880-0500, USA.

Abstract

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.

PMID:
10230612
DOI:
10.1016/s0960-894x(99)00113-4
[Indexed for MEDLINE]

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