Inhibition of Aldose Reductases from Rabbit Lens by Oxazole Derivatives
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概要
- 論文の詳細を見る
Twenty kinds of oxazole derivatives having various substituents at the C-2 and C-5 positions were synthesized and tested in vitro for inhibition of rabbit lens aldose reductase (Ia and Ib), the enzyme that initiates cataract formation in diabetes. Compounds possessing bulky groups at C-2 and C-5 of the oxazole skeleton were found to be potent inhibitors. Benzyl 5-phenyl-2-oxazolecarbamate (12) inhibited aldose reductases Ia and Ib by 50% at about 15μM. N-Phenyl-N'-(5-phenyl-2-oxazolyl) urea also exhibited inhibitory activity comparable to that of compound 12. The structure-inhibitory activity relationships are discussed.
- 公益社団法人日本薬学会の論文
- 1984-03-25
著者
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田中 千秋
Osaka University of Pharmaceutical Sciences
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谷本 剛
Division of Biological Chemistry and Reference Standards, National Institute of Hygienic Sciences
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川村 次良
Division of Biological Chemistry and Reference Standards, National Institute of Hygienic Sciences
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福田 秀男
National Institute of Hygienic Sciences
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福田 秀男
Division of Biological Chemistry and Reference Standards, National Institute of Hygienic Sciences
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中尾 ますみ
Osaka College of Pharmacy
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福田 秀男
Division Of Biological Chemistry And Reference Standards National Institute Of Hygienic Sciences
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田中 千秋
Osaka College Of Pharmacy
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谷本 剛
国立衛生試験所大阪支所薬品試験部
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島田 詩子
Osaka College of Pharmacy
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山田 晃
Osaka College of Pharmacy
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谷本 剛
Division Of Biological Chemistry And Biologicals National Institute Of Hygienic Sciences
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