Your browser version may not work well with NCBI's Web applications. More information here...
1: Bioorg Med Chem Lett. 2005 Dec 1;15(23):5211-7. Epub 2005 Oct 3.Click here to read Links

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

Chemistry Research and Discovery, Amgen Inc., One Amgen Center Dr., Thousand Oaks, CA 91320, USA. nxi@amgen.com

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.

PMID: 16203144 [PubMed - indexed for MEDLINE]