title: Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives.
abstract: The paper covers continuing efforts to discover novel, potent and selective oxytocin antagonists. Further benzofuran derivatives with potent oxytocin antagonist activity and good pharmacokinetic parameters are reported. Efforts to improve the in vivo activity of the series are described.
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: Christopher J
authors: CJ
authors: Gardner
authors: David G
authors: DG
authors: Livermore
authors: Jackie E
authors: JE
authors: Mordaunt
authors: Fabrizio
authors: F
authors: Nerozzi
authors: Mamta
authors: M
authors: Patel
authors: Marion J
authors: MJ
authors: Perren
authors: Gordon G
authors: GG
authors: Weingarten
authors: Shalia
authors: S
authors: Shabbir
authors: Patrick M
authors: PM
authors: Woollard
authors: Ping
authors: P
authors: Zhou
mesh_terms: D000818:Animals; D001572:Benzofurans / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D015195:Drug Design; D005260:Female; D006801:Humans; D007700:Kinetics; D008958:Models, Molecular; D008968:Molecular Conformation; D010121:Oxytocin / Q000037:antagonists & inhibitors*; D051381:Rats; D018045:Receptors, Oxytocin / Q000037:antagonists & inhibitors / Q000378:metabolism; D013329:Structure-Activity Relationship; D014590:Uterine Contraction / Q000187:drug effects
chemical_list: D001572:Benzofurans; D018045:Receptors, Oxytocin; D010121:Oxytocin