Na^+-Glucose Cotransporter Inhibitors as Antidiabetic Agents. III. Synthesis and Pharmacological Properties of 4'-Dehydroxyphlorizin Derivatives Modified at the OH Groups of the Glucose Moiety
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概要
- 論文の詳細を見る
To overcome hydrolysis by β-glucosidase persent in the digestive tract, the OH groups on the glucose moiety of the 4'-dehydroxyphlorizin derivatives (1,2,3) were modified with various kinds of patterns, and then the effects of the modified compounds on urinary glucose excretion were evaluated in rats. Among them, triacetyl (9), , 2,3-O-diacetyl (17), 6-O-methoxycarbonyl (34), 4-O-methoxycarbonyl (38), and 2-O-acetyl (41) derivatives showed more potent effect than the parent compound 2 by oral administration (p.o.). The stabilities of the compounds 34,38,and 41 against β-glucosidase were higher than that of 2. The increase in oral activity was found to correlate with the enhancement of the stability against β-glucosidase.
- 公益社団法人日本薬学会の論文
- 1998-10-15
著者
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Matsumoto M
Osaka Medical Center For Cancer And Cardiovascular Diseases Osaka
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Matsumoto Misako
Department Of Immunology Osaka Medical Center For Cancer And Cardiovascular Diseases
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TSUDA Kinsuke
Laboratory of Metabolism, Graduate School of Human and Environmental Studies, Kyoto University
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ARAKAWA Kenji
Discovery Research Laboratory, Tanabe Seiyaku Co., Ltd.
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Matsumoto Mitsuharu
Takeda Chemical Industries Ltd. Pharmaceutical Research Division
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Kano-ishihara Tomomi
Discovery Research Laboratory Tanabe Seiyaku Co. Ltd.
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YAMAKITA Hirokazu
Pharmaceutics Research Laboratory, Tanabe Seiyaku Co., Ltd.
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Funami Nobuyuki
Lead Optimization Research Laboratory Tanabe Seiyaku Co. Ltd.
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Tsujihara K
Discovery Research Laboratory Tanabe Seiyaku Co. Ltd.
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Hongu M
Lead Optimization Research Laboratory Tanabe Seiyaku Co. Ltd.
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HONGU Mitsuya
Discovery Research Laboratory, Tanabe Seiyaku Co. Ltd.,
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FUNAMI Nobuyuki
Discovery Research Laboratory, Tanabe Seiyaku Co. Ltd.,
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TAKAHASHI Youichi
Discovery Research Laboratory, Tanabe Seiyaku Co. Ltd.,
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SAITO Kunio
Discovery Research Laboratory, Tanabe Seiyaku Co. Ltd.,
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MATSUMOTO Mamoru
Discovery Research Laboratory, Tanabe Seiyaku Co. Ltd.,
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TSUJIHARA Kenji
Discovery Research Laboratory, Tanabe Seiyaku Co. Ltd.,
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Tsuda Kinsuke
Laboratory Of Metabolism Graduate School Of Human And Environmental Studies Kyoto University
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Tsuda Kinsuke
Graduate School Of Human Science Kyoto University
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Arakawa K
Pharmacology Research Laboratories Tanabe Seiyaku Co. Ltd.
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Tsuda Kinsuke
Kyoto Univ. Kyoto Jpn
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Matsumoto Mitsuhiro
First Department Of Internal Medicine Kumamoto University School Of Medicine
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Yamakita H
Pharmaceutics Research Laboratory Tanabe Seiyaku Co. Ltd.
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Yamakita Hirokazu
Pharmaceutics Research Laboratory Tanabe Seiyaku Co. Ltd.
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Takahashi Youichi
Discovery Research Laboratory Tanabe Seiyaku Co. Ltd.
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Saito K
Graduate School Of Pharmaceutical Sciences Chiba University
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Saito K
Saitama Institute Of Public Health
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Saito Kazuki
Faculty Of Pharmaceutical Sciences Laboratory Of Molecular Biology And Biotechnology Research Center
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