title: Design and optimization of potent, selective antagonists of Oxytocin.
abstract: A novel series of Oxytocin antagonists are described. This series was identified through pharmacophoric overlap of in-house and literature antagonists. Subsequent optimization led to a series of potent, selective antagonists. Several analogues displayed oral bioavailability in vivo in the rat.
authors.affiliation: Discovery Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. Alan.D.Brown@pfizer.com
authors.forename: Alan
authors.initials: A
authors.lastname: Brown
authors.forename: Lindsay
authors.initials: L
authors.lastname: Brown
authors.forename: Dave
authors.initials: D
authors.lastname: Ellis
authors.forename: Nicholas
authors.initials: N
authors.lastname: Puhalo
authors.forename: Chris R
authors.initials: CR
authors.lastname: Smith
authors.forename: Olga
authors.initials: O
authors.lastname: Wallace
authors.forename: Lesa
authors.initials: L
authors.lastname: Watson
mesh_terms: D000284:Administration, Oral; D000818:Animals; D020650:Combinatorial Chemistry Techniques; D015394:Molecular Structure; D010120:Oxytocics / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D010121:Oxytocin / Q000037:antagonists & inhibitors*; D051381:Rats; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D010120:Oxytocics; D014230:Triazoles; D010121:Oxytocin