Discovery of potent CRTh2 (DP2) receptor antagonists

Starting with the weak agonist indomethacin, a series of potent, selective CRTh2 (DP2) antagonists have been discovered as potential treatments for asthma, allergic rhinitis and other inflammatory diseases.

Graphical abstractThe discovery and optimisation of potent antagonists of the CRTh2 receptor is described culminating in the synthesis of 12, a novel, potent, selective and metabolically stable lead compound.Figure optionsDownload full-size imageDownload as PowerPoint slide