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ID: ALA1131664
Journal: Bioorg Med Chem Lett
Title: Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors.
Authors: Dominguez C, Duffy DE, Han Q, Alexander RS, Galemmo RA, Park JM, Wong PC, Amparo EC, Knabb RM, Luettgen J, Wexler RR.
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.
CiteXplore: 10230612