Benzenesulfonamide誘導体の合成とThromboxane A_2及びLeukotriene D_4に対するDual拮抗作用
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概要
- 論文の詳細を見る
In order to find dual antagonists against both thromboxane A_2 (TXA_2) and leukotriene D_4 (LTD_4) receptors for a new antiasthmatic agent, various benzenesulfonamide derivatives were synthesized and evaluated for those pharmacological effects. TXA_2 and LTD_4 antagonistic activities in vitro were evaluated by the inhibitory effects on LTD_4-induced and U-46619-induced contraction of guinea-pig trachea. Furthermore, TXA_2 and LTD_4 antagonistic activities in vivo were evaluated by the inhibitory effects on LTD_4-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-LTD_4 and anti-TXA_2 activities by oral administration.
- 社団法人日本薬学会の論文
- 1997-05-25
著者
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加藤 日出男
北陸製薬株式会社
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大橋 徹生
北陸製薬株式会社
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桜井 俊一郎
北陸製薬株式会社中央研究所研究開発本部
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小川 信男
北陸製薬株式会社中央研究所研究開発本部
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小野木 泰代
北陸製薬株式会社中央研究所研究開発本部
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加戸 典幸
北陸製薬株式会社中央研究所研究開発本部
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安田 信吾
北陸製薬株式会社中央研究所研究開発本部
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加藤 日出男
北陸製薬株式会社中央研究所
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