Recent advances in DNA gyrase-targeted antimicrobial agents

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 structureactivity relationship studies of the published inhibitors. (C) 2020 Elsevier Masson SAS. All rights reserved.