Identification and optimization of novel 1,3,4-oxadiazole EP1 receptor antagonists

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4450-5. doi: 10.1016/j.bmcl.2007.06.014. Epub 2007 Jun 8.

Abstract

A novel series of oxadiazole EP1 receptor antagonists was identified by replacing the amide of a known glycine sulfonamide derivative with a 1,3,4-oxadiazole. Optimization of the substitution patterns on the three aromatic rings led to the identification of high affinity EP1 receptor antagonists. The derivative with highest affinity displayed a binding IC50 of 2.5 nM (pIC50 8.6).

MeSH terms

  • Models, Molecular
  • Molecular Structure
  • Oxadiazoles / chemistry*
  • Oxadiazoles / pharmacology*
  • Protein Binding
  • Receptors, Prostaglandin E / antagonists & inhibitors*
  • Receptors, Prostaglandin E, EP1 Subtype
  • Structure-Activity Relationship

Substances

  • Oxadiazoles
  • Receptors, Prostaglandin E
  • Receptors, Prostaglandin E, EP1 Subtype