Indole-3-acetic Acid Antagonists of the Prostaglandin D2 Receptor CRTH2
| Autor: | Luzheng Xue, Mark Richard Ashton, Frederick Arthur Brookfield, Shân L. Gyles, Mark Cowley Whittaker, Roy Pettipher, Richard Edward Armer, Edward Andrew Boyd, Michael G. Hunter, Christopher James Brennan, Philip Andrew Hay, David Middlemiss, Lucien Gazi |
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| Rok vydání: | 2005 |
| Předmět: |
Receptors
Prostaglandin Biological Availability CHO Cells Pharmacology Structure-Activity Relationship chemistry.chemical_compound Cricetulus Cricetinae Drug Discovery medicine Animals Humans Sulfones Receptors Immunologic Receptor Asthma Prostaglandin D2 receptor Indoleacetic Acids Prostaglandin D2 Chemistry Anti-Inflammatory Agents Non-Steroidal Atopic dermatitis medicine.disease In vitro Rats Bioavailability Biochemistry Toxicity Molecular Medicine Calcium |
| Zdroj: | Journal of Medicinal Chemistry. 48:6174-6177 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm050519b |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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