Syntheses of 2-Mercapto-4-substituted Imidazole Derivatives with Antiinflammatory Properties
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概要
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Various 2-mercapto-4-substituted-5-imidazolecarboxylates (5) were synthesized by the reaction of C-acylamino acid methyl esters (4) with potassium thiocyanate. Hydrolysis followed by decarboxylation of the imidazole carboxylates (5) gave 2-mercapto-4-substituted imidazoles (8) in good yields. Furthermore, the imidazoles (8) were also directly obtained by the reaction of aminoketones (9) with potassium thiocyanate. These compounds (8) exhibited antiinflammatory activities against carrageenan-induced rat paw edema. Among the compounds tested, 2-mercapto-4-(3-thienyl) imidazole (8r) showed the best therapeutic index value, giving a value comparable to that of mefenamic acid.
- 社団法人日本薬学会の論文
- 1984-07-25
著者
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松本 和男
田辺製薬医薬育成所
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松本 和男
Research Laboratory Of Applied Biochemistry Tanabe Seiyaku Co. Ltd.
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鈴木 護
Research Laboratory of Applied Biochemistry, Tanabe Seiyaku Co., Ltd.,
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前田 貞夫
Research Laboratory of Applied Biochemistry, Tanabe Seiyaku Co., Ltd.,
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岩澤 義郎
Biological Research Laboratory, Tanabe Seiyaku Co., Ltd.,
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岩崎 為雄
Research Laboratory of Applied Biochemistry, Tanabe Seiyaku Co., Ltd.
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岩澤 義郎
Pharmacological Research Laboratory, Tanabe Seiyaku Co., Ltd.
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岩澤 義郎
Biological Research Laboratory Tanabe Seiyaku Co. Ltd.
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鈴木 護
Research Laboratory Of Applied Biochemistry Tanabe Seiyaku Co. Ltd.
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岩崎 為雄
Research Laboratories Of Tanabe Seiyaku Co. Ltd.
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前田 貞夫
Research Laboratory Of Applied Biochemistry Tanabe Seiyaku Co. Ltd.
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