Characterization of mono- and diaminopyrimidine derivatives as novel, nonpeptide gonadotropin releasing hormone (GnRH) receptor antagonists

被引：25

作者：

Luthin, DR ^{[1
]}

Hong, YF ^{[1
]}

Tompkins, E ^{[1
]}

Anderes, KL ^{[1
]}

Paderes, G ^{[1
]}

Kraynov, EA ^{[1
]}

Castro, MA ^{[1
]}

Nared-Hood, KD ^{[1
]}

Castillo, R ^{[1
]}

Gregory, M ^{[1
]}

Vazir, H ^{[1
]}

May, JM ^{[1
]}

Anderson, MB ^{[1
]}

机构：

[1] Agouron Pharmaceut Inc, Pfizer Global Res & Dev La Jolla, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 24期

关键词：

D O I：

10.1016/S0960-894X(02)00756-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of derivatives of mono- and diaminopyrimidines 1 potently displaced binding of a radiolabeled GnRH analogue to human and rat GnRH receptors. Analogues from these series competitively antagonized GnRH-stimulated increases in extracellular acidification in vitro and suppressed GnRH-mediated increases in circulating luteinizing hormone (LH) in castrated rats and testosterone in intact rats. These compounds or their analogues may be useful in treating sex hormone-dependent disease. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：3635 / 3639

页数：5

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