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ID: ALA1133798
Journal: Bioorg Med Chem Lett
Title: Potent and selective bicyclic lactam inhibitors of thrombin. Part 4: transition state inhibitors.
Authors: Bachand B, Tarazi M, St-Denis Y, Edmunds JJ, Winocour PD, Leblond L, Siddiqui MA.
Abstract: Bicyclic piperazinone based thrombin inhibitors of general structure 2 were prepared and evaluated in vitro and in vivo. These inhibitors, having in common an electrophilic basic trans-cyclohexylamine P1 residue, displayed high thrombin affinity, high selectivity against trypsin and good in vivo efficacy in the rat arterial thrombosis model.
CiteXplore: 11212093