Discovery of potent CRTh2 (DP2) receptor antagonists.
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.
Birkinshaw
Timothy N
TN
Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Loughborough, UK. tim.birkinshaw@astrazeneca.com
Teague
Simon J
SJ
Beech
Claire
C
Bonnert
Roger V
RV
Hill
Stephen
S
Patel
Anil
A
Reakes
Sara
S
Sanganee
Hitesh
H
Dougall
Iain G
IG
Phillips
Tim T
TT
Salter
Sylvia
S
Schmidt
Jerzy
J
Arrowsmith
Elizabeth C
EC
Carrillo
Juan J
JJ
Bell
Fiona M
FM
Paine
Stuart W
SW
Weaver
Richard
R
D001249:Asthma / Q000188:drug therapy*; D002626:Chemistry, Pharmaceutical; D015195:Drug Design; D006801:Humans; D007213:Indomethacin / Q000494:pharmacology*; D007249:Inflammation / Q000188:drug therapy*; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D011485:Protein Binding; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors*; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D012220:Rhinitis / Q000188:drug therapy*
D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; D007213:Indomethacin; C036293:prostaglandin D2 receptor