title: Initial structure-activity relationship studies of a novel series of pyrrolo[1,2-a]pyrimid-7-ones as GnRH receptor antagonists.
abstract: Initial SAR studies on 1-aminomethyl-2-aryl-3-cyano-pyrrolo[1,2-a]pyrimid-7-one-6-carboxylates as human GnRH receptor antagonists were discussed. 2-(2-Methylaminoethyl)pyridine was discovered to be a key feature for generating active compounds. The best compound from the series had 25 nM (K(i)) binding affinity to human GnRH receptor.
authors.affiliation: Neurocrine Biosciences, Inc., 10555 Science Center Drive, San Diego, CA 92121, USA. fzhu@neurocrine.com
authors.forename: Yun-Fei
authors.initials: YF
authors.lastname: Zhu
authors.forename: R Scott
authors.initials: RS
authors.lastname: Struthers
authors.forename: Patrick J
authors.initials: PJ
authors.lastname: Connors
authors.forename: Yinghong
authors.initials: Y
authors.lastname: Gao
authors.forename: Timothy D
authors.initials: TD
authors.lastname: Gross
authors.forename: John
authors.initials: J
authors.lastname: Saunders
authors.forename: Keith
authors.initials: K
authors.lastname: Wilcoxen
authors.forename: Greg J
authors.initials: GJ
authors.lastname: Reinhart
authors.forename: Nicholas
authors.initials: N
authors.lastname: Ling
authors.forename: Chen
authors.initials: C
authors.lastname: Chen
mesh_terms: D000818:Animals; D006801:Humans; D007202:Indicators and Reagents; D007700:Kinetics; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology*; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology*; D011869:Radioligand Assay; D051381:Rats; D011966:Receptors, LHRH / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D007202:Indicators and Reagents; D011744:Pyrimidinones; D011758:Pyrroles; D011966:Receptors, LHRH