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

…, NJ Ashweek, XJ Liu, RS Struthers, MJ Bradbury…

Index: 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 Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 14 p. 3845 - 3850

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Citation Number: 7

Abstract

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.