Identification of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-3-yl)-ethylamine derivatives as novel GnRH receptor antagonists |
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| Authors: | 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 |
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| Affiliation: | Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA. |
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| 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. |
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