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

被引：22
|
作者：
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
机构：
[1] BioChem Therapeut Inc, Laval, PQ H7V 4A7, Canada
[2] Warner Lambert Parke Davis, Parke Davis Pharmaceut Res, Ann Arbor, MI 48105 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 22期
关键词：
D O I：
10.1016/S0960-894X(98)00550-2
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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. (C) 1998 Elsevier Science Ltd. All rights reserved.
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页码：3193 / 3198
页数：6
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