title: Identification of amide bioisosteres of triazole oxytocin antagonists.
abstract: A series of amides were investigated as potential bioisosteres of previously reported triazole oxytocin antagonists. A range of potent analogues were identified, although SAR for potency and selectivity over the related V(1A) and V(2) receptors was found to be somewhat divergent from that observed for the corresponding triazole series. The high synthetic accessibility of this new amide series also facilitated the identification of a range of alternative left hand side (biaryl replacement) substituents which gave good levels of oxytocin antagonism.
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: D000577:Amides / Q000737:chemistry* / Q000494:pharmacology*; D065092:Antidiuretic Hormone Receptor Antagonists; D008958:Models, Molecular; D015394:Molecular Structure; D010121:Oxytocin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D017483:Receptors, Vasopressin / Q000378:metabolism; D014230:Triazoles / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000577:Amides; D065092:Antidiuretic Hormone Receptor Antagonists; D017483:Receptors, Vasopressin; D014230:Triazoles; D010121:Oxytocin