title: 2,5-Diketopiperazines as potent and selective oxytocin antagonists 1: Identification, stereochemistry and initial SAR.
abstract: This paper covers efforts to discover orally active potent and selective oxytocin antagonists. Screening pooled libraries identified a novel series of 2,5-diketopiperazine derivatives with antagonist activity at the human oxytocin receptor. We report the initial structure-activity relationship investigations and the determination of the stereochemistry of the most potent compounds.
authors.affiliation: Department of Medicinal Chemistry CVU UK, GlaxoSmithKline Research and Development Limited, Medicines Research Centre, Gunnels Wood Road, Stevenage, Herts SG1 2NY, UK.
authors.forename: Paul G
authors.initials: PG
authors.lastname: Wyatt
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Allen
authors.forename: Alan D
authors.initials: AD
authors.lastname: Borthwick
authors.forename: Dave E
authors.initials: DE
authors.lastname: Davies
authors.forename: Anne M
authors.initials: AM
authors.lastname: Exall
authors.forename: Richard J D
authors.initials: RJ
authors.lastname: Hatley
authors.forename: Wendy R
authors.initials: WR
authors.lastname: Irving
authors.forename: David G
authors.initials: DG
authors.lastname: Livermore
authors.forename: Neil D
authors.initials: ND
authors.lastname: Miller
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Nerozzi
authors.forename: Steve L
authors.initials: SL
authors.lastname: Sollis
authors.forename: Anna Katrin
authors.initials: AK
authors.lastname: Szardenings
mesh_terms: D006801:Humans; D010879:Piperazines / Q000737:chemistry* / Q000494:pharmacology*; D018045:Receptors, Oxytocin / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D010879:Piperazines; D018045:Receptors, Oxytocin