Identification of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-3-yl)-ethylamine derivatives as novel GnRH receptor antagonists
作者:Mi Chen、Zhiqiang Guo、Marion C. Lanier、Liren Zhao、Stephen F. Betz、Charles Q. Huang、Colin J. Loweth、Neil J. Ashweek、Xin-Jun Liu、R. Scott Struthers、Margaret J. Bradbury、James W. Behan、Jenny Wen、Zhihong O’Brien、John Saunders、Yun-Fei Zhu
DOI:10.1016/j.bmcl.2007.05.009
日期:2007.7
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.