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N-substituted piperazinyl sarafloxacin derivatives: synthesis and in vitro antibacterial evaluation

Ali Asadipour1,2, Mohammad Hassan Moshafi3, Leila Khosravani4

  • 1Department of Medicinal Chemistry, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran.

Daru : Journal of Faculty of Pharmacy, Tehran University of Medical Sciences
|November 5, 2018
PubMed
Abstract

Insights

Medicinal chemists developed new fluoroquinolone derivatives to combat resistant bacteria. Some compounds showed promising activity against Gram-positive bacteria, similar to existing treatments.

Area of Science:

  • Medicinal Chemistry
  • Antimicrobial Drug Discovery

Background:

  • Fluoroquinolones (FQs) are vital antimicrobial agents for various infections.
  • Increasing resistance necessitates the development of novel FQ-based compounds, particularly against Gram-positive bacteria.

Purpose of the Study:

  • To synthesize and evaluate new quinolone-based compounds for enhanced antibacterial activity.
  • To address the growing challenge of fluoroquinolone-resistant microbes.

Main Methods:

  • Synthesis of N-[2-(aryl-3-yl) ethyl] piperazinyl quinolone derivatives via a two-component reaction.
  • Evaluation of antibacterial activity against a panel of Gram-positive and Gram-negative bacteria using MIC values.

Main Results:

  • Twenty-four new compounds were synthesized and tested against reference strains.
  • Compound 4g demonstrated significant inhibitory activity against Gram-positive bacteria, comparable to sarafloxacin.
  • Benzyloxime derivatives generally showed weak activity, with an exception in compound 4x.

Conclusions:

  • The synthesized compounds with a substituted piperazine moiety at the C-7 position exhibited comparable or weaker activity than sarafloxacin.
  • Further research may be needed to optimize these structures for improved efficacy against resistant strains.
Keywords:
Antibacterial activityGram-positive bacteriaQuinolonesSynthesis

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