Novel bicyclic lactam inhibitors of thrombin: potency and selectivity optimization through P1 residues

S Levesque, Y St-Denis, B Bachand, P Preville…

文献索引：Levesque, Sophie; St-Denis, Yves; Bachand, Benoit; Preville, Patrice; Leblond, Lorraine; Winocour, Peter D; Edmunds, Jeremy J; Rubin; Siddiqui Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 24 p. 3161 - 3164

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被引用次数: 14

摘要

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.