Novel potent and selective Ca 2+ release-activated Ca 2+(CRAC) channel inhibitors. Part 3: Synthesis and CRAC channel inhibitory activity of 4′-[(trifluoromethyl) …

…, Y Okamoto, M Funatsu, N Yoshimura-Ishikawa…

Index: Yonetoku, Yasuhiro; Kubota, Hirokazu; Miyazaki, Yoji; Okamoto, Yoshinori; Funatsu, Masashi; Yoshimura-Ishikawa, Noriko; Ishikawa, Jun; Yoshino, Taiji; Takeuchi, Makoto; Ohta, Mitsuaki Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 21 p. 9457 - 9466

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Citation Number: 21

Abstract

From a series of 4'-[(trifluoromethyl) pyrazol-1-yl] carboxanilides derived from 4-methyl-4'-[3, 5-bis (trifluoromethyl)-1H-pyrazol-1-yl]-1, 2, 3-thiadiazole-5-carboxanilide, one inhibited thapsigargin-induced Ca2+ influx in Jurkat T cells (IC50= 77nM) and exhibited high selectivity for the CRAC channel over the VOC channel (index:> 130). Another acted as an inhibitor for both T lymphocyte activation-induced diseases and ovalbumin-induced ...