title: Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists.
abstract: A series of heterocyclic 2-(3,5-dimethylphenyl)tryptamine derivatives was prepared and evaluated on a rat gonadotropin releasing hormone receptor assay. The carbon tether length and heterocyclic ring attached to the amino group of 2-(3,5-dimethylphenyl)tryptamine were varied. Several of these derivatives were potent GnRH antagonists with the most potent compound having an IC50 of 16 nM.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. peter_lin@merck.com
authors.forename: P
authors.initials: P
authors.lastname: Lin
authors.forename: M
authors.initials: M
authors.lastname: Parikh
authors.forename: J L
authors.initials: JL
authors.lastname: Lo
authors.forename: Y T
authors.initials: YT
authors.lastname: Yang
authors.forename: K
authors.initials: K
authors.lastname: Cheng
authors.forename: R G
authors.initials: RG
authors.lastname: Smith
authors.forename: M H
authors.initials: MH
authors.lastname: Fisher
authors.forename: M J
authors.initials: MJ
authors.lastname: Wyvratt
authors.forename: M T
authors.initials: MT
authors.lastname: Goulet
mesh_terms: D000818:Animals; D001665:Binding Sites / Q000502:physiology; D015195:Drug Design; D005260:Female; D006571:Heterocyclic Compounds / Q000138:chemical synthesis*; D006727:Hormone Antagonists / Q000737:chemistry / Q000378:metabolism*; D020128:Inhibitory Concentration 50; D051381:Rats; D011966:Receptors, LHRH / Q000378:metabolism*; D014363:Tryptamines / Q000138:chemical synthesis* / Q000378:metabolism*
chemical_list: D006571:Heterocyclic Compounds; D006727:Hormone Antagonists; D011966:Receptors, LHRH; D014363:Tryptamines; C030820:tryptamine