title: Identification of potent and selective oxytocin antagonists. Part 1: indole and benzofuran derivatives.
abstract: Studies to discover novel, potent and selective oxytocin antagonists are reported. Combinatorial libraries designed to find novel replacements of fragments of oxytocin antagonist L-371,257, identified pyrimidine, thiazole, indole and benzofuran as potential alternatives to the benzoic acid moiety of L-371,257. Additional investigations identified indole and benzofuran derivatives with potent oxytocin antagonist activity.
authors: Department of Medicinal Chemistry, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, SG1 2NY, Herts, UK.
authors: Paul G
authors: PG
authors: Wyatt
authors: Michael J
authors: MJ
authors: Allen
authors: Josie
authors: J
authors: Chilcott
authors: Alison
authors: A
authors: Foster
authors: David G
authors: DG
authors: Livermore
authors: Jackie E
authors: JE
authors: Mordaunt
authors: Jan
authors: J
authors: Scicinski
authors: Patrick M
authors: PM
authors: Woollard
mesh_terms: D000818:Animals; D001572:Benzofurans / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D001682:Biological Availability; D004285:Dogs; D015195:Drug Design; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D007700:Kinetics; D008958:Models, Molecular; D008968:Molecular Conformation; D010121:Oxytocin / Q000037:antagonists & inhibitors*; D018045:Receptors, Oxytocin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D001572:Benzofurans; D007211:Indoles; D018045:Receptors, Oxytocin; D010121:Oxytocin