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

被引：24

作者：

Xi, N ^{[1
]}

Bo, YX ^{[1
]}

Doherty, EM ^{[1
]}

Fotsch, C ^{[1
]}

Gavva, NR ^{[1
]}

Han, NH ^{[1
]}

Hungate, RW ^{[1
]}

Klionsky, L ^{[1
]}

Liu, QY ^{[1
]}

Tamir, R ^{[1
]}

Xu, S ^{[1
]}

Treanor, JJS ^{[1
]}

Norman, MH ^{[1
]}

机构：

[1] Amgen Inc, Dept Neurosci, Thousand Oaks, CA 91320 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 23期

关键词：

vanilloid receptor 1 (TRPV1); antagonists; thiazole carboxamides;

D O I：

10.1016/j.bmcl.2005.08.100

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 mu M in these assays. (c) 2005 Elsevier Ltd. All rights reserved.

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收藏

页码：5211 / 5217

页数：7

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