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 ,
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.
