Background: In the past few decades, with the abuse of antibiotics, bacterial resistance has enhanced constantly. More and more super species of bacteria, which are seriously threatening human health, have been discovered. Developing novel antibacterial agents to overcome the drug-resistance is an urgent duty. We all know that blocking the information-transfer of bacterial DNA and RNA is one of the effective ways to inhibit bacterial growth. Therefore, as the indispensable enzyme for DNA replication and transcription, DNA gyrase is one of the important targets for bacterial inhibitors. Accordingly, many inhibitors of DNA gyrase have also been developed.

Methods: In this review, to highlight the recent progress in DNA gyrase inhibitors, the study in this field over the past three years (2017-2019) was summarized and organized based on their backbones or core moieties. Both of the subunits of DNA gyrase were taken into consideration.

Results: These DNA gyrase inhibitors have been classified based on their backbones or core moieties. After the comparison of the divided 14 categories, we could achieve some clues for future modification. In particular, we found that benzodiazepines and naphthalene heterocycles were the most common structures in the drug design. On the other hand, isopropyl and cyclopropyl have also been used in drug design, which provides more inspiration for the investigations. Except for GSK2140944, which has entered the phase III clinical trial stage, other compounds here were not fully promulgated with their optimal pharmacokinetic activity.

Conclusion: We briefly summed up the current situation and future challenges on this topic. Through the discussion of the design strategies and drug effect, we hope that this review can provide a focused direction for future researches.

背景：近几十年来，随着抗生素的滥用，细菌耐药性不断增强。越来越多的超级细菌被发现，严重威胁人类健康。开发新型抗菌剂以克服耐药性是一项紧迫的任务。众所周知，阻断细菌DNA和RNA的信息传递是抑制细菌生长的有效途径之一。因此，作为DNA复制和转录必不可少的酶，DNA促旋酶是细菌抑制剂的重要靶点之一。因此，还开发了许多DNA促旋酶抑制剂。

方法：在这篇综述中，为了突出 DNA 促旋酶抑制剂的最新进展，根据其骨架或核心部分总结和组织了过去三年（2017-2019）该领域的研究。DNA促旋酶的两个亚基都被考虑在内。

结果：这些 DNA 促旋酶抑制剂已根据其骨架或核心部分进行分类。经过对划分的14个类别的比较，我们可以为以后的修改找到一些线索。特别是，我们发现苯二氮卓类和萘杂环是药物设计中最常见的结构。另一方面，异丙基和环丙基也被用于药物设计，这为研究提供了更多的灵感。除了 GSK2140944 已进入 III 期临床试验阶段，这里的其他化合物并未完全公布其最佳药代动力学活性。

结论：我们简要总结了该主题的现状和未来挑战。通过对设计策略和药物效应的讨论，我们希望这篇综述能为未来的研究提供一个重点方向。