Recent advances in DNA gyrase-targeted antimicrobial agents

Eur J Med Chem. 2020 Aug 1:199:112326. doi: 10.1016/j.ejmech.2020.112326. Epub 2020 Apr 28.

Abstract

Antimicrobial resistance is one of the greatest challenges facing the world today. In the United States alone, it is responsible for the death of more than 20,000 people each year. DNA gyrase, a well-validated drug target, is involved in bacterial DNA replication, repair and decatenation. Currently, the fluoroquinolone class of antibacterials act via inhibition of the DNA gyrase enzyme. However, their efficacy is hindered by the increasing incidence of antimicrobial resistance. Therefore, in this review, we provide an account regarding the structure of DNA gyrase and quinoline and non-quinolone inhibitors published within the last five years (2015-2019). Further, we also discuss molecular interactions and structure-activity relationship studies of the published inhibitors.

Keywords: Antimicrobial; DNA gyrase; Fluoroquinolone.

Publication types

  • Review

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Bacteria / drug effects*
  • Bacteria / metabolism
  • DNA Gyrase / metabolism*
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Topoisomerase II Inhibitors / chemistry
  • Topoisomerase II Inhibitors / pharmacology*

Substances

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