Substituted indole-5-carboxamides and -acetamides as potent nonpeptide GnRH receptor antagonists

被引：41

作者：

Ashton, WT

Sisco, RM

Yang, YT

Lo, JL

Yudkovitz, JB

Cheng, K

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 / 13期

关键词：

D O I：

10.1016/S0960-894X(01)00274-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The 2-aryltryptamine class of GnRH receptor antagonists has been modified to incorporate carboxamide and acetamide substituents at the indole 5-position. With either a phenol or methanesulfonamide terminus on the N-aralkyl side chain, potent binding affinity to the GnRH receptor was achieved. A functional assay for GnRH antagonism was even more sensitive to structural modification and revealed a strong preference for branched tertiary amides. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：1723 / 1726

页数：4

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