Studies on Hypolipidemic Agents. V. Synthesis and Esterase-Inhibitory Activity of 2-(1,4- and 4,4-Dialkylcyclohexyl)-2-oxoethyl Arenesulfonates(Medicinal Chemistry,Chemical)
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概要
- 論文の詳細を見る
2-(1,t- and c-4-Dialkylcyclohex-r-1-yl)-2-oxoethyl arenesulfonates, 2-(4,4-dialkyleyclohex-1-yl)-2-oxoethyl arenesulfonates and related compounds were synthesized and evaluated for esteraseand chymotrypsin-inhibitory activities in vitro and for hypolipidemic effect in vivo. The transisomers of 2-(1,4-dialkylcyclohex-1-yl)-2-oxoethyl arenesulfonates showed much more potent esterase-inhibitory action (about 13 to 6200 times) than the cis-isomers as well as more potent hypolipidemic action (about 1.5 to 10 times) but the chymotrypsin-inhibitory actions of the two isomers were similarly low. On the other hand, the 2-oxoethyl arenesulfonates having a 4,4-disubstituted cyclohexane ring mostly exhibited potent esterase-inhibitory action (order of IC_<50>; 10^<-8> to 10^<-9> M) and marked hypolipidemic effect (78% to 95% reductions of plasma triglyceride).
- 社団法人日本薬学会の論文
- 1987-10-25
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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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
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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