Discovery of potent CRTh2 (DP2) receptor antagonists

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4287-90. doi: 10.1016/j.bmcl.2006.05.062. Epub 2006 Jun 5.

Abstract

Starting with the weak agonist indomethacin, a series of potent, selective CRTh2 (DP(2)) antagonists have been discovered as potential treatments for asthma, allergic rhinitis and other inflammatory diseases.

MeSH terms

  • Asthma / drug therapy*
  • Chemistry, Pharmaceutical
  • Drug Design
  • Humans
  • Indomethacin / pharmacology*
  • Inflammation / drug therapy*
  • Inhibitory Concentration 50
  • Models, Chemical
  • Protein Binding
  • Receptors, Immunologic / antagonists & inhibitors*
  • Receptors, Prostaglandin / antagonists & inhibitors*
  • Receptors, Prostaglandin / metabolism
  • Rhinitis / drug therapy*

Substances

  • Receptors, Immunologic
  • Receptors, Prostaglandin
  • Indomethacin
  • prostaglandin D2 receptor