Synthesis and structure-activity relationships of 1-arylmethyl-3(2-aminopropyl)-5-aryl-6-methyluracils as potent GnRH receptor antagonists

被引：20

作者：

Guo, ZQ

Zhu, YF

Tucci, FC

Gao, YH

Struthers, RS

Saunders, J

Gross, TD

Xie, Q

Reinhart, GJ

Chen, C

机构：

[1] Neurocrine Biosci Inc, Dept Med Chem, San Diego, CA 92121 USA

[2] Neurocrine Biosci Inc, Dept Exploratory Discovery, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 19期

关键词：

D O I：

10.1016/S0960-894X(03)00620-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The novel synthesis and SAR studies of 6-methyluracils as human GnRH receptor antagonists are discussed. Introduction of a small methyl substituent at the beta-position from N3 of the uracil improved the GnRH binding potency by 5- to 10-fold. The best compound from the series had binding affinity of 5 nM (K-i) to the human GnRH receptor. (C) 2003 Elsevier Ltd. All rights reserved.

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页码：3311 / 3315

页数：5

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