Studies on 5-Lipoxygenase Inhibitors. I. Synthesis and 5-Lipoxygenase-Inhibitory Activity of Novel Hydroxamic Acid Derivatives
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概要
- 論文の詳細を見る
A series of novel hydroxamates has been prepared and tested for inhibitory activity towards rat polymorphonuclear leukocyte (PMN) 5-lipoxygenase (5-LO) in vitro and towards neutrophil migration in the rat air pouch model of inflammation in vivo. Many 3,4-dihydronaphthyl compounds were potent inhibitors of 5-LO, and several compounds were potent inhibitors of neutrophil migration. The most potent 3,4-dihydronaphthyl compound, N-[[(3,4-dihydro-5-phenoxy)-2-naphthyl]methyl]-N-hydroxy-N'-ethylurea (FR122788,18) had an IC_<50> of 25 nM in the 5-LO assay, and strongly reduced neutrophil migration in the rat air pouch model at 1 mg/kg (p.o.). FR122788 also had an ameliorating effect in a rat hepatiatis model induced by D-galactosamine, with an ED<50> values of 14.6 mg/kg (p.o.) for glutamate oxaloacetate transaminase (GOT) and 16.8 mg/kg (p.o.) for glutamate pyruvate transaminase (GPT).
- 公益社団法人日本薬学会の論文
- 1998-06-15
著者
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Tanaka H
Faculty Of Pharmacy Meijo University
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TANAKA Hirokazu
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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Oku Teruaki
Department Of Microbiology Hoshi University School Of Pharmacy And Pharmaceutical Sciences
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Oku Teruaki
Department Of Microbiology School Of Pharmacy Hoshi University
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Toyama Hirohide
Institute For Chemical Research Kyoto University
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Tanaka Haruyuki
Chemical Branch Faculty Of Engineering And Kansai University High Technology Research Center Kansai
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Oku T
Amagasaki Chemical Industries Co.
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Kawai Yoshio
Faculty Of Life Sciences Toyo University
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YATABE Takumi
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
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KAWAI Yoshio
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
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OKU Teruo
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
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Yatabe Takumi
Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Tanaka Hirokazu
Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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TANAKA Hiromi
Department of Physics Faculty of Education, Saga University
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