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. 2005 Dec 1;15(23):5211-7.
doi: 10.1016/j.bmcl.2005.08.100. Epub 2005 Oct 3.

Synthesis and evaluation of thiazole carboxamides as vanilloid receptor 1 (TRPV1) antagonists

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Synthesis and evaluation of thiazole carboxamides as vanilloid receptor 1 (TRPV1) antagonists

Ning Xi et al. Bioorg Med Chem Lett. .

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.

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