title: The discovery of GSK221149A: a potent and selective oxytocin antagonist.
abstract: Optimisation of a series of oxazole diketopiperazines has led to the discovery of a very potent and selective oxytocin antagonist GSK221149A. GSK221149A has been shown to inhibit oxytocin-induced uterine contractions in the anaesthetised rat.
authors.affiliation: Department of Medicinal Chemistry, GlaxoSmithKline Research and Development, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, UK. john.2.liddle@gsk.com
authors.forename: John
authors.initials: J
authors.lastname: Liddle
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Allen
authors.forename: Alan D
authors.initials: AD
authors.lastname: Borthwick
authors.forename: David P
authors.initials: DP
authors.lastname: Brooks
authors.forename: David E
authors.initials: DE
authors.lastname: Davies
authors.forename: Richard M
authors.initials: RM
authors.lastname: Edwards
authors.forename: Anne M
authors.initials: AM
authors.lastname: Exall
authors.forename: Chris
authors.initials: C
authors.lastname: Hamlett
authors.forename: Wendy R
authors.initials: WR
authors.lastname: Irving
authors.forename: Andrew M
authors.initials: AM
authors.lastname: Mason
authors.forename: Gerald P
authors.initials: GP
authors.lastname: McCafferty
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Nerozzi
authors.forename: Simon
authors.initials: S
authors.lastname: Peace
authors.forename: Joanne
authors.initials: J
authors.lastname: Philp
authors.forename: Derek
authors.initials: D
authors.lastname: Pollard
authors.forename: Mark A
authors.initials: MA
authors.lastname: Pullen
authors.forename: Shaila S
authors.initials: SS
authors.lastname: Shabbir
authors.forename: Steve L
authors.initials: SL
authors.lastname: Sollis
authors.forename: Timothy D
authors.initials: TD
authors.lastname: Westfall
authors.forename: Pat M
authors.initials: PM
authors.lastname: Woollard
authors.forename: Charlene
authors.initials: C
authors.lastname: Wu
authors.forename: Deirdre M B
authors.initials: DM
authors.lastname: Hickey
mesh_terms: D000818:Animals; D005260:Female; D006801:Humans; D007700:Kinetics; D010121:Oxytocin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D010879:Piperazines / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D018045:Receptors, Oxytocin / Q000378:metabolism; D013329:Structure-Activity Relationship; D014590:Uterine Contraction / Q000187:drug effects
chemical_list: C522194:GSK221149A; D010879:Piperazines; D018045:Receptors, Oxytocin; D010121:Oxytocin