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Identification of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-3-yl)-ethylamine derivatives as novel GnRH receptor antagonists. 2007
Mi Chen, and
Zhiqiang Guo, and
Marion C Lanier, and
Liren Zhao, and
Stephen F Betz, and
Charles Q Huang, and
Colin J Loweth, and
Neil J Ashweek, and
Xin-Jun Liu, and
R Scott Struthers, and
Margaret J Bradbury, and
James W Behan, and
Jenny Wen, and
Zhihong O'Brien, and
John Saunders, and
Yun-Fei Zhu
Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
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.
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Colin J Loweth, and
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