title: Identification of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-3-yl)-ethylamine derivatives as novel GnRH receptor antagonists.
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.
authors.affiliation: Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
authors.forename: Mi
authors.initials: M
authors.lastname: Chen
authors.forename: Zhiqiang
authors.initials: Z
authors.lastname: Guo
authors.forename: Marion C
authors.initials: MC
authors.lastname: Lanier
authors.forename: Liren
authors.initials: L
authors.lastname: Zhao
authors.forename: Stephen F
authors.initials: SF
authors.lastname: Betz
authors.forename: Charles Q
authors.initials: CQ
authors.lastname: Huang
authors.forename: Colin J
authors.initials: CJ
authors.lastname: Loweth
authors.forename: Neil J
authors.initials: NJ
authors.lastname: Ashweek
authors.forename: Xin-Jun
authors.initials: XJ
authors.lastname: Liu
authors.forename: R Scott
authors.initials: RS
authors.lastname: Struthers
authors.forename: Margaret J
authors.initials: MJ
authors.lastname: Bradbury
authors.forename: James W
authors.initials: JW
authors.lastname: Behan
authors.forename: Jenny
authors.initials: J
authors.lastname: Wen
authors.forename: Zhihong
authors.initials: Z
authors.lastname: O'Brien
authors.forename: John
authors.initials: J
authors.lastname: Saunders
authors.forename: Yun-Fei
authors.initials: YF
authors.lastname: Zhu
mesh_terms: 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
chemical_list: D011725:Pyridines; D011966:Receptors, LHRH; C023666:pyridine