The antibacterial activity of fluoroquinolone derivatives: An update (2018-2021)

Eur J Med Chem. 2021 Nov 15:224:113741. doi: 10.1016/j.ejmech.2021.113741. Epub 2021 Aug 2.

Abstract

Bacterial infection is amongst the most common diseases in community and hospital settings. Fluoroquinolones, exerting the antibacterial activity through binding to type II bacterial topoisomerase enzymes, DNA gyrase and topoisomerase IV, are mainstays of chemotherapy. At present, fluoroquinolones are the most valuable antibacterial agents used popularly. However, the emergence of more virulent and resistant pathogens by the development of either mutated DNA-binding proteins or efflux pump mechanism for fluoroquinolones results in an urgent demand to develop new fluoroquinolones to withstand the drug resistance and to obtain a broader spectrum of activity. This review aims to outline the recent advances of fluoroquinolone derivatives with antibacterial potential and to summarize the structure-activity relationship (SAR) so as to provide an insight for rational design of more active candidates, covering articles published between January 2018 and June 2021.

Keywords: Antibacterial; Drug resistance; Fluoroquinolone; Multidrug-resistant bacteria; Structure-activity relationship.

Publication types

  • Historical Article
  • Review

MeSH terms

  • Anti-Bacterial Agents / pharmacology
  • Anti-Bacterial Agents / therapeutic use*
  • Bacteria / drug effects*
  • Bacterial Infections / drug therapy*
  • Fluoroquinolones / pharmacology
  • Fluoroquinolones / therapeutic use*
  • History, 21st Century
  • Humans
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Fluoroquinolones