Abstract
A thiazole derivative, 2-(2,6-dichlorobenzyl)-N-(4-isopropylphenyl) thiazole-4-carboxamide (1), was identified as a TRPV1 antagonist. We synthesized various thiazole analogs and evaluated them for their ability to block capsaicin- or acid-induced calcium influx in TRPV1-expressing CHO cells. The IC(50) values of the most potent antagonists were ca. 0.050microM in these assays.
MeSH terms
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Amides / chemical synthesis
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Amides / chemistry*
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Amides / pharmacology*
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Animals
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CHO Cells
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Cricetinae
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Cricetulus
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Humans
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Molecular Structure
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Oxamic Acid / chemical synthesis
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Oxamic Acid / chemistry
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Oxamic Acid / pharmacology
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Structure-Activity Relationship
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TRPV Cation Channels / antagonists & inhibitors*
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Thiazoles / chemical synthesis
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Thiazoles / chemistry*
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Thiazoles / pharmacology*
Substances
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Amides
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TRPV Cation Channels
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TRPV1 protein, human
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Thiazoles
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Oxamic Acid