title: Identification of a urea bioisostere of a triazole oxytocin antagonist.
abstract: A series of azetidine ureas were investigated as potential bioisosteres of previously reported azetidinyltriazole oxytocin antagonists. Although potency was somewhat reduced in several close-in analogues, one compound, 9, was both a potent oxytocin antagonist and demonstrated significant selectivity over the closely related vasopressin V(1A) receptor.
authors.affiliation: Discovery Chemistry, Pfizer Global Research and Development, Sandwich, United Kingdom. Alan.D.Brown@pfizer.com
authors.forename: Alan
authors.initials: A
authors.lastname: Brown
authors.forename: Dave
authors.initials: D
authors.lastname: Ellis
authors.forename: Olga
authors.initials: O
authors.lastname: Wallace
authors.forename: Michael
authors.initials: M
authors.lastname: Ralph
mesh_terms: D008958:Models, Molecular; D010121:Oxytocin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry* / Q000494:pharmacology; D014508:Urea / Q000737:chemistry*
chemical_list: D014230:Triazoles; D010121:Oxytocin; D014508:Urea