- Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2.
Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2.
Journal of medicinal chemistry (2005-09-30)
Richard E Armer, Mark R Ashton, Edward A Boyd, Chris J Brennan, Frederick A Brookfield, Lucien Gazi, Shân L Gyles, Philip A Hay, Michael G Hunter, David Middlemiss, Mark Whittaker, Luzheng Xue, Roy Pettipher
PMID16190744
摘要
Prostaglandin D2 (PGD2) acting at the CRTH2 receptor (chemoattractant receptor-homologous molecule expressed on Th2 cells) has been linked with a variety of allergic and other inflammatory diseases. We describe a family of indole-1-sulfonyl-3-acetic acids that are potent and selective CRTH2 antagonists that possess good oral bioavailability. The compounds may serve as novel starting points for the development of treatments of inflammatory disease such as asthma, allergic rhinitis, and atopic dermatitis.