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

作者信息

St-Denis Y, Augelli-Szafran C E, Bachand B, Berryman K A, DiMaio J, Doherty A M, Edmunds J J, Leblond L, Lévesque S, Narasimhan L S, Penvose-Yi J R, Rubin J R, Tarazi M, Winocour P D, Siddiqui M A

机构信息

BioChem Therapeutic Inc., Laval, Québec, Canada.

出版信息

Bioorg Med Chem Lett. 1998 Nov 17;8(22):3193-8. doi: 10.1016/s0960-894x(98)00550-2.

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.

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