Discovery of CP-533536: an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation

Bioorg Med Chem Lett. 2009 Apr 1;19(7):2075-8. doi: 10.1016/j.bmcl.2009.01.059. Epub 2009 Jan 23.

Abstract

Sulfonamides, exemplified by 3a, were identified as highly selective EP(2) agonists. Lead optimization led to the identification of CP-533536, 7f, a potent and selective EP(2) agonist. CP-533536 demonstrated the ability to heal fractures when administered locally as a single dose in rat models of fracture healing.

MeSH terms

  • Animals
  • Male
  • Osteogenesis / drug effects*
  • Pyridines / administration & dosage
  • Pyridines / chemistry*
  • Pyridines / pharmacokinetics
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Prostaglandin E / agonists*
  • Receptors, Prostaglandin E / metabolism
  • Receptors, Prostaglandin E, EP2 Subtype
  • Structure-Activity Relationship
  • Sulfonamides / chemical synthesis
  • Sulfonamides / chemistry
  • Sulfonamides / pharmacology

Substances

  • CP533536
  • Ptger2 protein, rat
  • Pyridines
  • Receptors, Prostaglandin E
  • Receptors, Prostaglandin E, EP2 Subtype
  • Sulfonamides