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ID: ALA1130670

Journal: Bioorg Med Chem Lett

Title: Potent bicyclic lactam inhibitors of thrombin: Part I: P3 modifications.

Authors: St-Denis Y, Augelli-Szafran CE, Bachand B, Berryman KA, DiMaio J, Doherty AM, Edmunds JJ, Leblond L, Lévesque S, Narasimhan LS, Penvose-Yi JR, Rubin JR, Tarazi M, Winocour PD, Siddiqui MA.

Abstract: Peptidomimetic inhibitors of general structure 1 have been prepared. Optimization of the binding affinities of these compounds through variation of the P3 hydrophobic residue is described. Selected substituted bicylic lactams displayed interesting pharmacological profiles both in vitro and in vivo.

CiteXplore: 9873701

DOI: 10.1016/s0960-894x(98)00550-2