Studies on Prodrugs. IV. Preparation and Characterization of N-(5-Substituted 2-oxo-l,3-dioxol-4-yl)methyl Norfloxacin

Fumio Sakamoto, Shoji Ikeda, Hirosato Kondo, Goro Tsukamoto

研究成果: Contribution to journalArticle査読

28 被引用数 (Scopus)

抄録

As a new type of norfloxacin (NFLX) prodrug, N-(5-substituted 2-oxo-l, 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-l,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-l,3-dioxol-4-yl)methyl group was confirmed to function as an amine-type promoiety.

本文言語英語
ページ(範囲)4870-4877
ページ数8
ジャーナルChemical and Pharmaceutical Bulletin
33
11
DOI
出版ステータス出版済み - 1985
外部発表はい

All Science Journal Classification (ASJC) codes

  • 化学 (全般)
  • 創薬

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