Studis on Topical Antiinflammatory Agents. III. : Synthesis of 17α-Acyloxy-9α-fluoro-11β-hydroxy-16β-methyl-1,4-pregnadiene-3,20-dione 21-Thio Dericatives and Related Compounds
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概要
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A series of 21-thio derivatives of 9α-fluoro-11β, 17α-dihydroxy-16β-methyl-1,4-pregnadiene-3,20-dione 17-esters and related compounds were synthesized and evaluated as topical antiinflammatory agents. These compounds were prepared by the reaction of 9α-fluoro-11β, 17α, 21-trihydroxy-16β-methyl-1,4-pregnadiene-3,20-dione (betamethasone, I) 17-ester derivatives and various mercapto compounds. A structure-activity relationship study revealed that the structural combination of a thio group at the 21-position and an ester group at the 17-position contributed to vasoconstrictive activity. Among these compounds, the 21-methylthio 17-propanoate compound (6) was found to have the most potent activity, being more potent than betamethasone 17-valerate (BV).
- 公益社団法人日本薬学会の論文
- 1989-12-25
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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曽田 馨
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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曽田 馨
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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