Studies on Topical Antiinflammatory Agents. V. : 17-(Alkylthio)- and Methoxyalkanoates of Corticosteroids
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概要
- 論文の詳細を見る
As part of our search for new topical antiinflammatory agents, a series of corticosteroid 17-(alkylthio)- and methoxyalkanoate derivatives was prepared and tested for vasoconstrictive activities. Several compounds were proved to have activity superior or comparable to that of 9α-fluoro-11β, 21-dihydroxy-16β-methyl-17α-valeryloxy-1,4-pregnadiene-3,20-dione (betamethasone 17-valerate, BV). Among these compounds, 21-chloro-11β-hydroxy-17α-(methylthio)acetoxy-4-pregnene-3,20-dione (5Aa) was found to have the most potent activity, being more active than BV. The structure-activity relationships of the series revealed that introduction of a (methylthio)acetate function into the 17-position as well as the 21-position of corticosteroids was effective for enhancing the topical antiinflammatory activity.
- 公益社団法人日本薬学会の論文
- 1990-03-25
著者
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安井 一
Research Center Taisho Pharmaceutical Co. Ltd.
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畑山 勝男
Research Center, Taisho Pharmaceutical Co., Ltd.,
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畑山 勝男
Research Center Taisho Pharmaceutical Co. Ltd.
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樋口 昭平
Research Center Taisho Pharmaceutical Co. Ltd.
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三口 守公
Research Center, Taisho Pharmaceutical Co., Ltd.,
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池本 知之
Research Center, Taisho Pharmaceutical Co., Ltd.,
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田口 稔
Research Center, Taisho Pharmaceutical Co., Ltd.,
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阿部 訓志
Research Center, Taisho Pharmaceutical Co., Ltd.,
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田口 稔
Research Center Taisho Pharmaceutical Co. Ltd.
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池本 知之
Research Center Taisho Pharmaceutical Co. Ltd.
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三口 守公
Research Center Taisho Pharmaceutical Co. Ltd.
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阿部 訓志
Research Center Taisho Pharmaceutical Co. Ltd.
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Hatayama K
Research Center Taisho Pharmaceutical Co. Ltd.
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