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ID: ALA1134153
Journal: Bioorg Med Chem Lett
Title: Novel bicyclic lactam inhibitors of thrombin: potency and selectivity optimization through P1 residues.
Authors: Lévesque S, St-Denis Y, Bachand B, Préville P, Leblond L, Winocour PD, Edmunds JJ, Rubin JR, Siddiqui MA.
Abstract: Peptidomimetic inhibitors of thrombin lacking the important Ser195-carbonyl interaction have been prepared. The binding energy lost after the removal of the activated carbonyl was recaptured through a series of modifications of the P1 residues of the bicyclic lactam inhibitors. Selected substituted compounds displayed useful pharmacological profiles both in vitro and in vivo.
CiteXplore: 11720865