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    Bioorg Med Chem Lett. 2005 Dec 1;15(23):5211-7. Epub 2005 Oct 3.

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

    Xi N, Bo Y, Doherty EM, Fotsch C, Gavva NR, Han N, Hungate RW, Klionsky L, Liu Q, Tamir R, Xu S, Treanor JJ, Norman MH.

    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]

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