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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.

Original publication

DOI

10.1021/jm050519b

Type

Journal article

Journal

J Med Chem

Publication Date

06/10/2005

Volume

48

Pages

6174 - 6177

Keywords

Animals, Anti-Inflammatory Agents, Non-Steroidal, Biological Availability, CHO Cells, Calcium, Cricetinae, Cricetulus, Humans, Indoleacetic Acids, Prostaglandin D2, Rats, Receptors, Immunologic, Receptors, Prostaglandin, Structure-Activity Relationship, Sulfones