Title of article
Novel potent and selective Ca2+ release-activated Ca2+ (CRAC) channel inhibitors. Part 3: Synthesis and CRAC channel inhibitory activity of 4′-[(trifluoromethyl)pyrazol-1-yl]carboxanilides Original Research Article
Author/Authors
Yasuhiro Yonetoku، نويسنده , , Hirokazu Kubota، نويسنده , , Yoji Miyazaki، نويسنده , , Yoshinori Okamoto، نويسنده , , Masashi Funatsu، نويسنده , , Noriko Yoshimura-Ishikawa، نويسنده , , Jun Ishikawa، نويسنده , , Taiji Yoshino، نويسنده , , Makoto Takeuchi، نويسنده , , Mitsuaki Ohta، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
10
From page
9457
To page
9466
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 = 77 nM) 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 airway eosinophilia in rats (ED50 = 1.3 mg/kg) p.o.
Keywords
CRAC channel , Interleukin-2 , Anti-inflammatory , Channel inhibitors , Ca2+ release-activated Ca2+ channel
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2008
Journal title
Bioorganic and Medicinal Chemistry
Record number
1306974
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