Abstract
High throughput screening identified a 7-azaindole-3-acetic acid scaffold as a novel CRTh2 receptor antagonist chemotype, which could be optimised to furnish a highly selective compound with good functional potency for inhibition of human eosinophil shape change in whole blood and oral bioavailability in the rat.
MeSH terms
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Acetates / chemical synthesis
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Acetates / chemistry*
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Acetates / pharmacokinetics
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Administration, Oral
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Animals
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Anti-Inflammatory Agents / chemical synthesis
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Anti-Inflammatory Agents / chemistry*
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Anti-Inflammatory Agents / pharmacokinetics
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Eosinophils / drug effects
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Eosinophils / immunology
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Humans
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Microsomes, Liver / metabolism
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Permeability
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Pyridines / chemical synthesis
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Pyridines / chemistry*
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Pyridines / pharmacokinetics
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Rats
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Receptors, Immunologic / antagonists & inhibitors*
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Receptors, Immunologic / metabolism
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Receptors, Prostaglandin / antagonists & inhibitors*
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Receptors, Prostaglandin / metabolism
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Structure-Activity Relationship
Substances
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1H-pyrrolo(2,3-b)pyridine-3-acetic acid
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Acetates
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Anti-Inflammatory Agents
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Pyridines
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Receptors, Immunologic
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Receptors, Prostaglandin
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prostaglandin D2 receptor