Title of article
Novel potent and selective calcium-release-activated calcium (CRAC) channel inhibitors. Part 1: Synthesis and inhibitory activity of 5-(1-methyl-3-trifluoromethyl-1H-pyrazol-5-yl)-2-thiophenecarboxamides Original Research Article
Author/Authors
Yasuhiro Yonetoku، نويسنده , , Hirokazu Kubota، نويسنده , , Yoshinori Okamoto، نويسنده , , Akira Toyoshima، نويسنده , , Masashi Funatsu، نويسنده , , Jun Ishikawa، نويسنده , , Makoto Takeuchi، نويسنده , , Mitsuaki Ohta، نويسنده , , Shin-ichi Tsukamoto، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
11
From page
4750
To page
4760
Abstract
We synthesized and evaluated a series of 5-(1-methyl-3-trifluoromethyl-1H-pyrazol-5-yl)-2-thiophenecarboxamides to identify potent inhibitors of calcium-release-activated calcium (CRAC) channels with greater selectivity than voltage-operated calcium (VOC) channels. These efforts resulted in identification of compounds 22 and 24. The former exhibits highly potent and selective CRAC channel inhibitory activity, and the latter inhibited phytohemagglutinin-induced interleukin-2 production by Jurkat T lymphocytes and concanavalin A-induced hepatitis in mice.
Keywords
Indole and indazole benzyl ureas , TRPV1 antagonists
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2006
Journal title
Bioorganic and Medicinal Chemistry
Record number
1303678
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