New developments in non-quinolone-based antibiotics for the inhibiton of bacterial gyrase and topoisomerase IV

Eur J Med Chem. 2018 May 25:152:393-400. doi: 10.1016/j.ejmech.2018.04.059. Epub 2018 May 1.

Abstract

The inhibition of pathogenic bacteria at the replication stage is important to halt their further reproduction and spread. The replication enzymes include the DNA gyrase and topoisomerase IV that are recognized targets for the infection control. Novel antibiotic compounds are always in demand for targeting different active sites of these enzymes. Although quinolones are the current drug of choice for targeting these enzymes, emerging resistance is a global concern. Wide-scale efforts are needed to overcome the emerging resistance by designing more potent drugs. In this article, we have reviewed the last five years progress of various classes of non-quinolone-based chemical compounds that are tested for their antibacterial activities.

Keywords: Bacterial gyrase; Binding sites; Drug resistance; Potency; Topoisomerase IV.

Publication types

  • Review

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • DNA Gyrase / metabolism*
  • DNA Topoisomerase IV / antagonists & inhibitors*
  • DNA Topoisomerase IV / metabolism
  • Dose-Response Relationship, Drug
  • Humans
  • Molecular Structure
  • Staphylococcus aureus / enzymology
  • Structure-Activity Relationship
  • Topoisomerase Inhibitors / chemical synthesis
  • Topoisomerase Inhibitors / chemistry
  • Topoisomerase Inhibitors / pharmacology*

Substances

  • Anti-Bacterial Agents
  • Topoisomerase Inhibitors
  • DNA Topoisomerase IV
  • DNA Gyrase