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

EJ Iwanowicz, WF Lau, J Lin, DGM Roberts…

Index: Iwanowicz, Edwin J.; Lau, Wan F.; Lin, James; Roberts, Daniel G. M.; Seiler, Steven M. Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 12 p. 1339 - 1344

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Citation Number: 26

Abstract

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-α-thrombin complex. These analogs display competitive kinetics for the inhibition of human α-thrombin. The most potent member of this series 17, shows marked potency for thrombin with an inhibition constant, Ki of 260 nM.