Piperazinealkanol Ester Derivatives of Indomethacin as Dual Inhibitors of 5-Lipoxygenase and Cyclooxygenase
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概要
- 論文の詳細を見る
Piperazinealkanol ester derivatives of indomethacin were prepared and tested for inhibitory activities against 5-lipoxygenase (5-LO) and cyclooxygenase (CO). They inhibited 5-hydroxyeicosatetraenoic acid (5-HETE) formation by the cytosol of guinea pig polymorphonuclear leukocytes and thromboxane B_2 (TXB_2) formation by washed rabit platelet suspension. Of the test compounds, 2-[4-(2-hydroxyethyl)-1-piperazinyl]-1-phenylethyl 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-3-indolylacetate dimaleate (II-8) was found to be the most active dual inhibitor of 5-LO and CO, and its inhibitory potency was higher than that of 2-[4-(3-hydroxypropyl)-1-piperazinyl]-ethyl [1-(4-chlorobenzoyl)-5-methoxy-2-methyl]-3-indolylacetate (CR-1015) (I), the lead compound.
- 社団法人日本薬学会の論文
- 1994-04-15
著者
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鈴木 雅博
Hanno Research Center Chemistry Lab. Taiho Pharmaceutical Co. Ltd.
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山脇 一郎
Tokushima Research Center, Pharmacokinetics Research Lab., Taiho Pharmaceutical Co., Ltd.,
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小川 和男
Tokushima Research Center, Pharmacokinetics Research Lab., Taiho Pharmaceutical Co., Ltd.,
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小川 和男
Faculty Of Pharmaceutical Sciences Kanazawa University
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小川 和男
Tokushima Research Center Pharmacokinetics Research Lab. Taiho Pharmaceutical Co. Ltd.
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山脇 一郎
Tokushima Research Center Pharmacokinetics Research Lab. Taiho Pharmaceutical Co. Ltd.
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