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Inhibitors of Bacterial DNA Synthesis01:28

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Bacterial pathogens depend on precise and efficient DNA replication to sustain infection. Two type II topoisomerases—DNA gyrase and topoisomerase IV—are critical to this process, as they resolve DNA supercoiling and unlink chromosomes during replication. Fluoroquinolones, synthetic derivatives of quinolones, exploit this mechanism by stabilizing the transient DNA–enzyme cleavage complex, preventing strand religation, and causing lethal double-strand breaks. These antibiotics are selectively...
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Isolation and Identification of Waterborne Antibiotic-Resistant Bacteria and Molecular Characterization of their Antibiotic Resistance Genes
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Isolation and Identification of Waterborne Antibiotic-Resistant Bacteria and Molecular Characterization of their Antibiotic Resistance Genes

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Quinolone resistance.

J C Brown1, S G Amyes

  • 1Department of Medical Microbiology, Uiversity of Edinburgh Medical School, Edinburgh, UK.

Methods in Molecular Medicine
|March 11, 2011
PubMed
Summary
This summary is machine-generated.

Quinolone antibacterials, starting with nalidixic acid, treat infections. Newer fluoroquinolones offer potent activity against resistant bacteria, including serious infections.

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Area of Science:

  • Microbiology
  • Pharmacology
  • Infectious Diseases

Background:

  • Quinolone antibacterial agents were introduced in the early 1960s, with nalidixic acid being the first clinically used.
  • Nalidixic acid was effective for enteric and urinary tract infections but faced declining use due to clinical resistance.
  • The emergence of resistance spurred the development of more potent fluoroquinolones.

Purpose of the Study:

  • To review the development and clinical significance of quinolone antibacterial agents.
  • To highlight the advantages of fluoroquinolones over earlier quinolones.
  • To underscore the broad-spectrum efficacy and favorable pharmacokinetic properties of fluoroquinolones.

Main Methods:

  • Historical review of quinolone antibacterial development.
  • Analysis of clinical applications and resistance patterns.
  • Comparison of activity and properties between nalidixic acid and fluoroquinolones.

Main Results:

  • Fluoroquinolones exhibit antimicrobial activity up to one thousand times greater than nalidixic acid.
  • Bacteria resistant to early quinolones remain susceptible to fluoroquinolones.
  • Fluoroquinolones like ciprofloxacin and ofloxacin are effective against a wide range of bacterial infections, from UTIs to septicemia.

Conclusions:

  • Fluoroquinolones represent a significant advancement in antibacterial therapy.
  • Their broad spectrum of activity, unique mechanism, and favorable pharmacokinetics contribute to their clinical success.
  • These agents are crucial for treating diverse bacterial infections globally.