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Novel potent and selective calcium-release-activated calcium (CRAC) channel inhibitors. Part 2: Synthesis and inhibitory activity of aryl-3-trifluoromethylpyrazoles

Y Yonetoku, H Kubota, Y Okamoto, J Ishikawa…

文献索引:Yonetoku, Yasuhiro; Kubota, Hirokazu; Okamoto, Yoshinori; Ishikawa, Jun; Takeuchi, Makoto; Ohta, Mitsuaki; Tsukamoto, Shin-ichi Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 15 p. 5370 - 5383

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被引用次数: 41

摘要

To identify potent and selective calcium-release-activated calcium (CRAC) 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 ...