Abstract
DNA gyrase and topoisomerase IV are validated targets for developing dual-targeting antibacterial agents. The development of novel molecules targeting both enzymes has gained tremendous importance in circumventing the development of bacterial resistance. In the present review, we highlight the recent developments and discovery of dual-targeting inhibitors over the last five years. The structure-activity relationships, molecular docking analysis, and pharmacological activity are presented to facilitate the rational design and development of novel dual-targeting inhibitors to bridge the gap in antibiotic drug discovery.