Abstract
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.
MeSH terms
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
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Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology
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Biological Availability
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CHO Cells
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Calcium / metabolism
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Cricetinae
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Cricetulus
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Humans
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Indoleacetic Acids / chemical synthesis*
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Indoleacetic Acids / pharmacokinetics
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Indoleacetic Acids / pharmacology
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Prostaglandin D2 / pharmacology
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Rats
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Receptors, Immunologic / antagonists & inhibitors*
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Receptors, Prostaglandin / antagonists & inhibitors*
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Structure-Activity Relationship
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Sulfones / chemical synthesis
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Sulfones / pharmacokinetics
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Sulfones / pharmacology
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Indoleacetic Acids
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Receptors, Immunologic
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Receptors, Prostaglandin
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Sulfones
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indoleacetic acid
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Prostaglandin D2
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Calcium
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prostaglandin D2 receptor