Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 14, Issue 14, Pages 4750-4760Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2006.03.024
Keywords
anti-inflammatory; channel inhibitors; Ca2+-release-activated Ca2+ channel; CRAC channel; interleukin-2; quantitative structure-activity relationship
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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. (c) 2006 Elsevier Ltd. All rights reserved.
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