Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 2: (3-Substituted-5-halo-2-pyridinyl)guanidines

被引:18
作者
Barber, CG [1 ]
Dickinson, RP [1 ]
机构
[1] Pfizer Ltd, Global Res & Dev, Dept Discovery Chem, Sandwich CT13 9NJ, Kent, England
关键词
D O I
10.1016/S0960-894X(01)00702-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Based on previous modeling predictions, a series of (3-substituted-5-chloro-2-pyridinyl)guanidines have been designed with good potency and selectivity for urokinase-type plasminogen activator (uPA). Compound 3 has a K-i of 0.17 muM and greater than 300-fold selectivity with respect to tPA and plasmin (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:185 / 187
页数:3
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