| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1367719 | Bioorganic & Medicinal Chemistry Letters | 2005 | 7 Pages |
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 IC50 values of the most potent antagonists were ca. 0.050 μM in these assays.
Graphical abstractA series of thiazole carboxamides was prepared and evaluated as TRPV1 receptor antagonists. IC50 values of ca. 0.050 mM were achieved in either capsaicin- or acid-mediated calcium influx assays in TRPV1-expressing CHO cells.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Ning Xi, Yunxin Bo, Elizabeth M. Doherty, Christopher Fotsch, Narender R. Gavva, Nianhe Han, Randall W. Hungate, Lana Klionsky, Qingyian Liu, Rami Tamir, Shimin Xu, James J.S. Treanor, Mark H. Norman,