title: Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.
abstract: Structure-activity studies on the oxytocin antagonist 1 (L-371,257; Ki = 9.3 nM) have led to the identification of a related series of compounds containing an ortho-trifluoroethoxyphenylacetyl core which are orally bioavailable and have significantly improved potency in vitro and in vivo, e.g., compound 8 (L-374,943; Ki = 1.4 nM).
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA.
authors.forename: P D
authors.initials: PD
authors.lastname: Williams
authors.forename: M G
authors.initials: MG
authors.lastname: Bock
authors.forename: B E
authors.initials: BE
authors.lastname: Evans
authors.forename: R M
authors.initials: RM
authors.lastname: Freidinger
authors.forename: S N
authors.initials: SN
authors.lastname: Gallicchio
authors.forename: M T
authors.initials: MT
authors.lastname: Guidotti
authors.forename: M A
authors.initials: MA
authors.lastname: Jacobson
authors.forename: M S
authors.initials: MS
authors.lastname: Kuo
authors.forename: M R
authors.initials: MR
authors.lastname: Levy
authors.forename: E V
authors.initials: EV
authors.lastname: Lis
authors.forename: S R
authors.initials: SR
authors.lastname: Michelson
authors.forename: J M
authors.initials: JM
authors.lastname: Pawluczyk
authors.forename: D S
authors.initials: DS
authors.lastname: Perlow
authors.forename: D J
authors.initials: DJ
authors.lastname: Pettibone
authors.forename: A G
authors.initials: AG
authors.lastname: Quigley
authors.forename: D R
authors.initials: DR
authors.lastname: Reiss
authors.forename: C
authors.initials: C
authors.lastname: Salvatore
authors.forename: K J
authors.initials: KJ
authors.lastname: Stauffer
authors.forename: C J
authors.initials: CJ
authors.lastname: Woyden
mesh_terms: D000818:Animals; D048588:Benzoxazines; D002460:Cell Line; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D010078:Oxazines / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D010121:Oxytocin / Q000037:antagonists & inhibitors*; D010880:Piperidines / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D048588:Benzoxazines; C096766:L 371257; D010078:Oxazines; D010880:Piperidines; D010121:Oxytocin