Identification of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-3-yl)-ethylamine derivatives as novel GnRH receptor antagonists.
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.
Chen
Mi
M
Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
Guo
Zhiqiang
Z
Lanier
Marion C
MC
Zhao
Liren
L
Betz
Stephen F
SF
Huang
Charles Q
CQ
Loweth
Colin J
CJ
Ashweek
Neil J
NJ
Liu
Xin-Jun
XJ
Struthers
R Scott
RS
Bradbury
Margaret J
MJ
Behan
James W
JW
Wen
Jenny
J
O'Brien
Zhihong
Z
Saunders
John
J
Zhu
Yun-Fei
YF
D000818:Animals; D002478:Cells, Cultured; D006801:Humans; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D011966:Receptors, LHRH / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D011725:Pyridines; D011966:Receptors, LHRH; C023666:pyridine