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.
Kimberly O Cameron  1 ,  Bruce A Lefker ,  Hua Z Ke ,  Mei Li ,  Michael P Zawistoski ,  Christina M Tjoa ,  Ann S Wright ,  Shari L DeNinno ,  Vishwas M Paralkar ,  Thomas A Owen ,  Li Yu ,  David D Thompson
Affiliations
  • 1. Department of Cardiovascular and Metabolic Diseases, Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA. [email protected]
PMID: 19250823 DOI: 10.1016/j.bmcl.2009.01.059
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.

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