Title of article :
Identification of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-3-yl)-ethylamine derivatives as novel GnRH receptor antagonists
Author/Authors :
Chin-Mi Chen، نويسنده , , Zhiqiang Guo، نويسنده , , Marion C. Lanier، نويسنده , , Liren Zhao، نويسنده , , Stephen F. Betz، نويسنده , , Charles Q. Huang، نويسنده , , Colin J. Loweth، نويسنده , , Neil J. Ashweek، نويسنده , , Xin-Jun Liu، نويسنده , , R. Scott Struthers، نويسنده , , Margaret J. Bradbury، نويسنده , , James W. Behan، نويسنده , , Jenny Wen، نويسنده , , Zhihong O’Brien، نويسنده , , John Saunders، نويسنده , , Yun-Fei Zhu، نويسنده ,
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.
Keywords :
Non-peptide GnRH receptor antagonists , 5 , 6 , 2-c]pyridin-3-yl)-ethylamine , 12-(4
