Studies on Prodrugs. IV. Preparation and Characterization of N-(5-Substituted 2-oxo-1,3-dioxol-4-yl) methyl Norfloxacin
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概要
- 論文の詳細を見る
As a new type of norfloxacin (NFLX) prodrug, N-(5-substituted 2-oxo-1,3-dioxol-4-yl) methyl NFLXs were designed. These N-masked NFLXs were prepared and confirmed to produce higher NFLX levels in blood than NFLX itself after oral administration to mice. N-(5-Methyl-2-oxo-1,3-dioxol-4-yl) methyl NFLX was found to be smoothly hydrolyzed in mouse blood in vitro, and when administered orally, gave about 5-fold higher blood levels of NFLX than NFLX itself. Thus, the (5-methyl-2-oxo-1,3-dioxol-4-yl) methyl group was confirmed to function as an amine-type promoiety.
- 公益社団法人日本薬学会の論文
- 1985-11-25
著者
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塚本 悟郎
Pharmaceuticals Research Center, Kanebo Ltd.
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池田 昇司
Pharmaceuticals Reseach Center Kanebo Ltd.
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池田 昇司
Pharmaceuticals Research Center Kanebo Ltd.
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塚本 悟郎
New Drug Research Laboratories Kanebo Ltd.
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坂本 文夫
Pharmaceuticals Reseach Center, Kanebo Ltd.,
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坂本 文夫
Pharmaceuticals Research Center Kanebo Co. Ltd.
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近藤 裕郷
Pharmaceuticals Research Center Kanebo Co. Ltd.
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塚本 悟郎
Pharmaceutical Research Laboratory, Tanabe Seiyaku Co., Ltd.
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