Synthesis of Antimicrobial Agents. 3. Syntheses and Antibacterial Activities of 7-(4-Hydroxypiperazin-1-yl)quinolones

Toshio Uno, Hirosato Kondo, Yoshimasa Inoue, Yoshihiro Kawahata, Mikio Sotomura, Koji Iuchi, Goro Tsukamoto

研究成果: Contribution to journalArticle査読

15 被引用数 (Scopus)

抄録

A series of novel pyridone carboxylic acids having a 4-hydroxypiperazinyl group at the 7-position of norfloxacin and ciprofloxacin were prepared. The in vivo antibacterial efficacies of these compounds were superior to those of corresponding piperazinyl derivatives. From the results of the studies on the pharmacokinetic profile and toxicity, the 4-hydroxypiperazinyl derivatives were confirmed to be pharmacologically superior to corresponding piperazinyl derivatives. Thus, a 4-hydroxypiperazinyl group was revealed to be a beneficial substituent for potential use in future quinolone antibacterials.

本文言語英語
ページ(範囲)2929-2932
ページ数4
ジャーナルJournal of Medicinal Chemistry
33
10
DOI
出版ステータス出版済み - 10 1990
外部発表はい

All Science Journal Classification (ASJC) codes

  • 分子医療
  • 創薬

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