YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
Benzenesulfonamide誘導体の合成とThromboxane A2及びLeukotriene D4に対するDual拮抗作用
桜井 俊一郎小川 信男小野木 泰代大橋 徹生加戸 典幸安田 信吾加藤 日出男
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1997 年 117 巻 5 号 p. 298-318

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In order to find dual antagonists against both thromboxane A2 (TXA2) and leukotriene D4 (LTD4) receptors for a new antiasthmatic agent, various benzenesulfonamide derivatives were synthesized and evaluated for those pharmacological effects. TXA2 and LTD4 antagonistic activities in vitro were evaluated by the inhibitory effects on LTD4-induced and U-46619-induced contraction of guinea-pig trachea. Furthermore, TXA2 and LTD4 antagonistic activities in vivo were evaluated by the inhibitory effects on LTD4-induced and U-46619-induced bronchoconstriction of guinea-pig after oral administration of test compounds. It was found that 4-[5-[1-(4-chlorobenzenesulfonamido)-5-methylhexyl]-2-thienyl] butyric acid (12i) and 4-[5-[1-(4-fluorobenzenesulfonamido)-5-methylhexyl]-2-thienyl] butyric acid (12j) possess good anti-LTD4 and anti-TXA2 activities by oral administration.

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