Abstract
A series of tetrahydroquinoline-derived inhibitors of the CRTH2 receptor was discovered by a high throughput screen. Optimization of these compounds for potency and pharmacokinetic properties led to the discovery of potent and orally bioavailable CRTH2 antagonists.
MeSH terms
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Anti-Allergic Agents / chemistry*
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Anti-Allergic Agents / pharmacokinetics
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Anti-Allergic Agents / pharmacology
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Cell Line
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Cell Shape / drug effects
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Drug Discovery
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Eosinophils / drug effects
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Eosinophils / immunology
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Humans
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Quinolines / chemistry*
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Quinolines / pharmacokinetics
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Quinolines / pharmacology
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Receptors, Immunologic / antagonists & inhibitors*
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Receptors, Prostaglandin / antagonists & inhibitors*
Substances
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Anti-Allergic Agents
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Quinolines
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Receptors, Immunologic
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Receptors, Prostaglandin
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1,2,3,4-tetrahydroquinoline
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prostaglandin D2 receptor