Lactams as prostanoid receptor ligands. Part 4: 2-Piperidones as selective EP4 receptor agonists

Bioorg Med Chem Lett. 2005 May 16;15(10):2523-6. doi: 10.1016/j.bmcl.2005.03.059.

Abstract

2-Piperidones were prepared bearing heptanoic acid or a thioether heptanoic acid at the 1-position as well as appropriately substituted at the 6-position to mimic the structure of prostaglandins. The stereochemical purity at the 6-position was determined to be 95% ee for an advanced synthetic intermediate. The 2-piperidones were identified as potent agonists at the EP4 prostanoid receptor. They displayed a high affinity (Ki 5-130 nM) at EP4 and subtype selectivity.

MeSH terms

  • Lactams / chemistry
  • Lactams / pharmacology*
  • Ligands
  • Piperidones / chemistry
  • Piperidones / pharmacology*
  • Receptors, Prostaglandin E / agonists*
  • Receptors, Prostaglandin E, EP4 Subtype

Substances

  • Lactams
  • Ligands
  • Piperidones
  • Receptors, Prostaglandin E
  • Receptors, Prostaglandin E, EP4 Subtype