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

Authors :: Xi, Ning
Bo, Yunxin
Doherty, Elizabeth M.
Fotsch, Christopher
Gavva, Narender R.
Han, Nianhe
Hungate, Randall W.
Klionsky, Lana
Liu, Qingyian
Tamir, Rami
Xu, Shimin
Treanor, James J.S.
Norman, Mark H.
Source :: Bioorganic & Medicinal Chemistry Letters. Dec2005, Vol. 15 Issue 23, p5211-5217. 7p.
Publication Year :: 2005
Abstract: 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. 0.050μM in these assays. [Copyright &y& Elsevier]

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