Structure-activity relationship of biaryl acylsulfonamide analogues on the human EP(3) prostanoid receptor

Bioorg Med Chem Lett. 2002 Sep 16;12(18):2583-6. doi: 10.1016/s0960-894x(02)00518-8.


Potent and selective ligands for the human EP3 prostanoid receptor are described. Biaryl compounds bearing a tethered ortho substituted acidic moiety were identified as potent EP3 antagonists based on the SAR described herein. The binding affinity of key compounds on all eight human prostanoid receptors is reported.

MeSH terms

  • Humans
  • Receptors, Prostaglandin E / drug effects*
  • Receptors, Prostaglandin E, EP3 Subtype
  • Structure-Activity Relationship
  • Sulfonamides / chemistry*
  • Sulfonamides / pharmacology*


  • PTGER3 protein, human
  • Receptors, Prostaglandin E
  • Receptors, Prostaglandin E, EP3 Subtype
  • Sulfonamides