The emergence of bacterial resistance against life-saving medicines has forced the scientific community and pharmaceutical industry to take actions in the quest for novel antibacterials. These should not only overcome the existing bacterial resistance but also provide at least interim effective protection against emerging bacterial infections. Research into DNA gyrase and topoisomerase IV inhibitors has become a particular focus, with the description of a new class of bacterial topoisomerase type II inhibitors known as “novel bacterial topoisomerase inhibitors”, NBTIs. Elucidation of the key structural modifications incorporated into these inhibitors and the impact these can have on their general physicochemical properties are detailed in this review. This defines novel bacterial topoisomerase inhibitors with promising antibacterial activities and potencies, which thus represent one potential example of the future “drugs for bad bugs”, as identified by the World Health Organization.

中文翻译：

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新型细菌拓扑异构酶抑制剂（NBTI）的SAR成功故事已有两个十年。

对救生药物的细菌抗药性的出现迫使科学界和制药业采取行动寻求新型抗菌剂。这些不仅应克服现有的细菌抗性，而且还应至少提供针对新兴细菌感染的临时有效保护。DNA促旋酶和拓扑异构酶IV抑制剂的研究已成为特别关注的领域，描述了一类称为“新型细菌拓扑异构酶抑制剂”的新型细菌拓扑异构酶II抑制剂NBTI。本综述详细阐明了这些抑制剂中所含的关键结构修饰及其对它们的一般物理化学性质的影响。