Studies on Antidiabetic Agents. IX. : A New Aldose Reductase Inhibitor, AD-5467,and Related 1,4-Benzoxazine and 1,4-Benzothiazine Derivatives : Synthesis and Biological Activity
スポンサーリンク
概要
- 論文の詳細を見る
N-Acetic acid derivatives (I) of 2-substituted 1,4-benzoxazines and benzothiazines were designed and synthesized for evaluation as new aldose reductase inhibitors. In general, 3-thioxo derivatives were more potent inhibitors of aldose reductase from human placenta in vitro than the corresponding 3-oxo derivatives. While many compounds (I) were not very effective in inhibiting sorbitol accumulation in the rat sciatic nerve in vivo, the 3-thioxo compounds bearing an isopropyl group at the 2-position showed highly potent activity in the in vivo assay. Compound 46 (AD-5467) was selected from this series as a candidate for further development.
- 社団法人日本薬学会の論文
- 1990-05-25
著者
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目黒 寛司
Chemistry Research Laboratories Research and Development Division, Takeda Chemical Industries, Ltd.
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多和田 紘之
Chemistry Research Laboratories Research and Development Division, Takeda Chemical Industries, Ltd.
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池田 衡
丸石製薬株式会社中央研究所
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目黒 寛司
浜理薬品工業株式会社
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杉山 泰雄
武田薬品工業株式会社 創薬研究本部
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杉山 泰雄
Biology Research Laboratories
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池田 衡
Biology Research Laboratories
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山本 佑二郎
Senju Pharmaceutical Co., Ltd.,
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Sugiyama Y
Takeda Chemical Industries Ltd. Pharmaceutical Research Division
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Sugiyama Y
Pharmaceutical Research Laboratories Ii Pharmaceutical Research Division Takeda Chemical Industries
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杉山 泰雄
武田薬品工業
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多和田 紘之
Pharmaceutical Research Laboratories Ii Pharmaceutical Research Division Takeda Chemical Industries
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Ikeda H
Fukuoka Univ. Fukuoka Jpn
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Mizuno K
Faculty Of Integrated Arts And Sciences The University Of Tokushima
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山本 佑二郎
Senju Pharmaceutical Co. Ltd.
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池田 衡
Biology Laboratories, Central Research Division, Takeda Chemical Industries, Ltd.
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