Abstract
The chemoattractant receptor-homologous molecule expressed on T(H)2 cells (CRTH-2), also found on eosinophils and basophils, is a prostaglandin D2 receptor involved in the recruitment of these cell types during an inflammatory response. In this report, we describe the synthesis and optimization of a ramatroban isostere that is a selective and potent antagonist of CRTH-2 which may be useful in the treatment of certain diseases.
MeSH terms
-
Anti-Asthmatic Agents / chemistry
-
Anti-Asthmatic Agents / pharmacology
-
Carbazoles / chemistry*
-
Carbazoles / pharmacology*
-
Isomerism
-
Models, Chemical
-
Molecular Conformation
-
Molecular Structure
-
Receptors, Immunologic / antagonists & inhibitors*
-
Receptors, Prostaglandin / antagonists & inhibitors*
-
Structure-Activity Relationship
-
Sulfonamides / chemistry*
-
Sulfonamides / pharmacology*
Substances
-
Anti-Asthmatic Agents
-
Carbazoles
-
Receptors, Immunologic
-
Receptors, Prostaglandin
-
Sulfonamides
-
ramatroban
-
prostaglandin D2 receptor