New class of biphenylene dibenzazocinones as potent ligands for the human EP1 prostanoid receptor

Bioorg Med Chem Lett. 1999 Sep 20;9(18):2699-704. doi: 10.1016/s0960-894x(99)00465-5.

Abstract

A new class of potent and selective ligands for the human EP1 prostanoid receptor is described. SAR studies reported herein allowed the identification of several potent dibenzazocinones bearing an acylsulfonamide side chain. The binding affinity of these compounds on all eight human prostanoid receptors is reported.

MeSH terms

  • Azocines / chemistry
  • Azocines / metabolism
  • Azocines / pharmacology*
  • Biphenyl Compounds / chemistry
  • Biphenyl Compounds / metabolism
  • Biphenyl Compounds / pharmacology*
  • Humans
  • Ligands
  • Protein Binding
  • Receptors, Prostaglandin E / drug effects*
  • Receptors, Prostaglandin E / metabolism
  • Receptors, Prostaglandin E, EP1 Subtype
  • Structure-Activity Relationship

Substances

  • Azocines
  • Biphenyl Compounds
  • Ligands
  • PTGER1 protein, human
  • Receptors, Prostaglandin E
  • Receptors, Prostaglandin E, EP1 Subtype