Initial structure-activity relationship of a novel class of nonpeptidyl GnRH receptor antagonists: 2-arylindoles

被引：50

作者：

Chu, L

Hutchins, JE

Weber, AE

Lo, JL

Yang, YT

Cheng, K

Smith, RG

Fisher, MH

Wyvratt, MJ

Goulet, MT

机构：

[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck Res Labs, Dept Biochem & Physiol, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(00)00707-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A nonpeptidyl GnRH receptor antagonist (1), with a unique 2-arylindole core, was identified through the Merck inhouse screening for binding affinity on the rat GnRH receptor. SAR studies directed toward the alkoxy-ethanolamine and 2-aryl groups resulted in a simpler lead structure with improved activity. This compound 50 exhibits a 60-fold improvement in binding activity over our initial lead 1. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：509 / 513

页数：5

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