7-Azaindole-3-acetic acid derivatives: Potent and selective CRTh2 receptor antagonists

Bioorganic & Medicinal Chemistry Letters(2009)

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摘要
High throughput screening identified a 7-azaindole-3-acetic acid scaffold 7 as a novel CRTh2 receptor antagonist chemotype, which could be optimised to furnish a highly selective compound 13l with good functional potency for inhibition of human eosinophil shape change in whole blood and oral bioavailability in the rat.
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关键词
CRTh2,Prostaglandin D2,Azaindole,Eosinophils,Allergic diseases
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