Identification of a urea bioisostere of a triazole oxytocin antagonist.
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.
Brown
Alan
A
Discovery Chemistry, Pfizer Global Research and Development, Sandwich, United Kingdom. Alan.D.Brown@pfizer.com
Ellis
Dave
D
Wallace
Olga
O
Ralph
Michael
M
D008958:Models, Molecular; D010121:Oxytocin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry* / Q000494:pharmacology; D014508:Urea / Q000737:chemistry*
D014230:Triazoles; D010121:Oxytocin; D014508:Urea