期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 14, 期 15, 页码 5370-5383出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2006.03.039
关键词
anti-inflammatory; channel inhibitors; Ca2+ release-activated Ca2+ channel; CRAC channel; interleukin-2; X-ray diffraction studies
To identify potent and selective calcium-release-activated calcium (CRAG) channel inhibitors, we examined the structure-activity relationships of the pyrazole and thiophene moieties in compound 4. Compound 25b was found to exhibit highly potent and selective inhibitory activity for CRAC channels and further modifications of the pyrazole and benzoyl moieties of compound 25b produced compound 29. These compounds were potent inhibitors of IL-2 production in vitro and also acted as inhibitors in pharmacological models of diseases resulting from T-lymphocyte activation, after oral administration. (c) 2006 Elsevier Ltd. All rights reserved.
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