Studies of Hypolipidemic Agents. I. : Syntheses and Hypolipidemic Activities of 1-Substituted 2-Alkanone Derivatives
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概要
- 論文の詳細を見る
Many 1-substituted 2-alkanone derivatives were synthesized and their inhibitory activities toward pancreatic lipase and esterase were examined in order to obtain hypolipidemic agents. 1-Benzenesulfonyloxy-2-pentanone (VI-2a) and 1-(2,4,6-trimethylbenzenesulfonyloxy)-2-pentanone (VI-2q) exhibited not only potent and selective esterase inhibitions (IC_<50> : 9.0×10^<-7>M and 1.0×10^<-6>M, respectively), but also potent hypolipidemic action (90 and 92% reductions of plasma triglyceride, and 53 and 90% reductions of plasma total cholesterol, respectively). A novel working hypothesis is presented to account for the lowering of the plasma lipids level, i.e., that inhibition of esterase and lipase activities in the small intestinal lumen may be responsible for the decrease in the plasma lipids level.
- 社団法人日本薬学会の論文
- 1986-03-25
著者
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寺田 忠史
Hanno Research Center, 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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橋本 貞夫
Research Laboratory, Taiho Pharmaceutical Co., Ltd.
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寺田 忠史
Hanno Research Center Taiho Pharmaceutical Co. Ltd.
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小川 和男
Research Institute, Taiho Pharmaceutical Co., Ltd.
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寺田 忠史
Research Institute, Taiho Pharmaceutical Co., Ltd.
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小川 和男
Faculty Of Pharmaceutical Sciences Kanazawa University
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村中 義幸
Research Institute, Taiho Pharmaceutical Co., Ltd.
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浜川 寿博
Research Institute, Taiho Pharmaceutical Co., Ltd.
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藤井 節郎
Institute for Protein Research, Osaka University
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村中 義幸
Research Institute Taiho Pharmaceutical Co.. Ltd.
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浜川 寿博
Research Institute Taiho Pharmaceutical Co.. Ltd.
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橋本 貞夫
Research Institute Taiho Pharmaceutical Co. Ltd.
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