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

Research output: Contribution to journalArticlepeer-review

12 Citations (Scopus)


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.

Original languageEnglish
Pages (from-to)2929-2932
Number of pages4
JournalJournal of Medicinal Chemistry
Issue number10
Publication statusPublished - Oct 1990
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery


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