Studies on Prodrugs. 5. Synthesis and Antimicrobial Activity of N-(Oxoalkyl)norfloxacin Derivatives

Hirosato Kondo, Fumio Sakamoto, Yasuo Kodera, Goro TsUKamoto

Research output: Contribution to journalArticle

38 Citations (Scopus)

Abstract

Several N-(oxoalkyl) norfloxacin derivatives (3a-g) were synthesized and evaluated for antibacterial activity in vitro and in vivo. Most of the compounds exhibited in vitro activity comparable to that of norfloxacin for Gram-positive bacteria, whereas their activity was lower than for Gram-negative bacteria. N-(2-Oxopropyl)norfloxacin (3b) liberated norfloxacin in the blood after oral administration in mice, and the serum level of norfloxacin was about 3-fold higher than that of norfloxacin itself. Thus, 3b showed high antibacterial activity in vivo.

Original languageEnglish
Pages (from-to)2020-2024
Number of pages5
JournalJournal of Medicinal Chemistry
Volume29
Issue number10
DOIs
Publication statusPublished - Jan 1 1986
Externally publishedYes

Fingerprint

Norfloxacin
Prodrugs
Gram-Positive Bacteria
Gram-Negative Bacteria
Oral Administration
Serum

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

Cite this

Studies on Prodrugs. 5. Synthesis and Antimicrobial Activity of N-(Oxoalkyl)norfloxacin Derivatives. / Kondo, Hirosato; Sakamoto, Fumio; Kodera, Yasuo; TsUKamoto, Goro.

In: Journal of Medicinal Chemistry, Vol. 29, No. 10, 01.01.1986, p. 2020-2024.

Research output: Contribution to journalArticle

Kondo, Hirosato ; Sakamoto, Fumio ; Kodera, Yasuo ; TsUKamoto, Goro. / Studies on Prodrugs. 5. Synthesis and Antimicrobial Activity of N-(Oxoalkyl)norfloxacin Derivatives. In: Journal of Medicinal Chemistry. 1986 ; Vol. 29, No. 10. pp. 2020-2024.
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