Discovery of a potent and selective agonist of the prostaglandin EP4 receptor

  • Bioorg Med Chem Lett. 2003 Mar 24;13(6):1129-32. doi: 10.1016/s0960-894x(03)00042-8.
Xavier Billot  1 ,  Anne Chateauneuf ,  Nathalie Chauret ,  Danielle Denis ,  Gillian Greig ,  Marie Claude Mathieu ,  Kathleen M Metters ,  Deborah M Slipetz ,  Robert N Young
Affiliations
  • 1. Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe Claire-Dorval, Québec, Canada H9R 4P8.
PMID: 12643927 DOI: 10.1016/s0960-894x(03)00042-8
Abstract

Analogues of PGE(2) wherein the hydroxycyclopentanone ring has been replaced by a lactam have been prepared and evaluated as ligands for the EP(4) receptor. An optimized compound (19a) shows high potency and agonist efficacy at the EP(4) receptor and is highly selective over the Other seven known prostaglandin receptors.

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