Identification of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-3-yl)-ethylamine derivatives as novel GnRH receptor antagonists

被引：7
|
作者：
Chen, Mi
Guo, Zhiqiang
Lanier, Marion C.
Zhao, Liren
Betz, Stephen F.
Huang, Charles Q.
Loweth, Colin J.
Ashweek, Neil J.
Liu, Xin-Jun
Struthers, R. Scott
Bradbury, Margaret J.
Behan, James W.
Wen, Jenny
O'Brien, Zhihong
Saunders, John
Zhu, Yun-Fei
机构：
[1] Neurocrine Biosci Inc, Dept Med Chem, San Diego, CA 92130 USA
[2] Neurocrine Biosci Inc, Dept Endocrinol, San Diego, CA 92130 USA
[3] Neurocrine Biosci Inc, Dept Neurosci, San Diego, CA 92130 USA
[4] Neurocrine Biosci Inc, Dept Preclin Dev, San Diego, CA 92130 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 14期
关键词：
non-peptide GnRH receptor antagonists; 12-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-3-yl)-ethylamine;
D O I：
10.1016/j.bmcl.2007.05.009
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A novel series of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-3-yl)-ethylamine derivatives were designed and synthesized as GnRH receptor antagonists. SAR studies led to a series of highly active molecules against both the rat and human receptors. Furthermore, one potent compound, 17j, demonstrated dose-dependent LH suppression in castrated rats. (C) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3845 / 3850
页数：6
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