Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-Isoquinolinylguanidines

被引：32

作者：

Barber, CG ^{[1
]}

Dickinson, RP ^{[1
]}

Fish, PV ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, Dept Discovery Chem, Sandwich CT13 9NJ, Kent, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 12期

关键词：

uPA; urokinase plasminogen activator; UK-356202; 1-isoquinolinylguanidine;

D O I：

10.1016/j.bmcl.2004.03.094

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 1-isoquinolinylguanidines are shown to be potent inhibitors of uPA with selectivity over tPA and plasmin. Potency is enhanced by the presence of a 4-halo and a 7-aryl substituent, particularly when substituted by a 3-carboxylic acid group. Compound 13j (UK-356,202) combines excellent potency and selectivity, and has been selected as a candidate for clinical evaluation. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：3227 / 3230

页数：4

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