Identification of a urea bioisostere of a triazole oxytocin antagonist

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1851-3. doi: 10.1016/j.bmcl.2010.01.143. Epub 2010 Feb 2.

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.

MeSH terms

  • Models, Molecular
  • Oxytocin / antagonists & inhibitors*
  • Structure-Activity Relationship
  • Triazoles / chemistry*
  • Triazoles / pharmacology
  • Urea / chemistry*

Substances

  • Triazoles
  • Oxytocin
  • Urea