Discovery of novel N-acylsulfonamide analogs as potent and selective EP3 receptor antagonists

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2639-43. doi: 10.1016/j.bmcl.2010.02.034. Epub 2010 Feb 13.


A series of novel N-acylsulfonamide analogs were synthesized and evaluated for their binding affinity and antagonist activity for the EP3 receptor subtype. Representative compounds were also evaluated for their inhibitory effect on PGE(2)-induced uterine contraction in pregnant rats. Among those tested, a series of N-acylbenzenesulfonamide analogs were found to be more potent than the corresponding carboxylic acid analogs in both the in vitro and in vivo evaluations. The structure activity relationships (SAR) are also discussed.

MeSH terms

  • Animals
  • Dinoprostone / pharmacology
  • Drug Discovery
  • Female
  • Pregnancy
  • Rats
  • Receptors, Prostaglandin E / antagonists & inhibitors*
  • Receptors, Prostaglandin E, EP3 Subtype
  • Structure-Activity Relationship
  • Sulfonamides / chemistry
  • Sulfonamides / pharmacology*
  • Uterine Contraction / drug effects


  • Receptors, Prostaglandin E
  • Receptors, Prostaglandin E, EP3 Subtype
  • Sulfonamides
  • Dinoprostone