Derivatives of 5-amidine indole as inhibitors of thrombin catalytic activity

被引：27

作者：

Iwanowicz, EJ

Lau, WF

Lin, J

Roberts, DGM

Seiler, SM

机构：

[1] Bristol-Myers Squibb P., Princeton

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 12期

关键词：

D O I：

10.1016/0960-894X(96)00229-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Substituted 5-amidine indoles were constructed based upon a computational analysis of putative modes of binding to thrombin utilizing coordinates from the crystal structure of BMS-183,507-alpha-thrombin complex. These analogs display competitive kinetics for the inhibition of human cr-thrombin. The most potent member of this series 17, shows marked potency for thrombin with an inhibition constant, K-i of 260 nM. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：1339 / 1344

页数：6

共 17 条

[1]

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[2]

BAGDY D, 1992, THROMB HAEMOSTASIS, V67, P357

[3]

BANNER DW, 1991, J BIOL CHEM, V266, P20085

[4]

BLANEY JM, DGEOM QUANTUM CHEM P