噻唑甲酰胺类作为香草酸受体1（TRPV1）拮抗剂的合成与评价
Synthesis and evaluation of thiazole carboxamides as vanilloid receptor 1 (TRPV1) antagonists.
作者信息
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
机构信息
Chemistry Research and Discovery, Amgen Inc., One Amgen Center Dr., Thousand Oaks, CA 91320, USA.
出版信息
Bioorg Med Chem Lett. 2005 Dec 1;15(23):5211-7. doi: 10.1016/j.bmcl.2005.08.100. Epub 2005 Oct 3.
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.
一种噻唑衍生物，2-(2,6-二氯苄基)-N-(4-异丙基苯基)噻唑-4-甲酰胺(1)，被鉴定为一种TRPV1拮抗剂。我们合成了各种噻唑类似物，并评估了它们阻断辣椒素或酸诱导的TRPV1表达的CHO细胞中钙内流的能力。在这些试验中，最有效的拮抗剂的IC(50)值约为0.050微摩尔。
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