Piperazinealkanol Ester Derivatives of Indomethacin as Dual Inhibitors of 5-Lipoxygenase and Cyclooxygenase

Ichiro YAMAWAKI; Masahiro SUZUKI; Kazuo OGAWA

doi:10.1248/cpb.42.963

著者情報

キーワード: piperazinealkanol ester derivative, indomethacin, dual inhibitor, 5-lipoxygenase, cyclooxygenase, 2-[4-(3-hydroxypropyl)-1-piperazinyl]-ethyl [1-(4-chlorobenzoyl)-5-methoxy-2-methyl]-3-indolylacetate

ジャーナルフリー

1994 年 42 巻 4 号 p. 963-971

DOI https://doi.org/10.1248/cpb.42.963

詳細

抄録

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 B₂ (TXB₂) 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.

責任著者(Corresponding author)

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