The search for new antimicrobials is imperative due to the emergent resistance of new microorganism strains. In this context, revisiting known classes like 8-hydroxyquinolines could be an interesting strategy to discover new agents. The 8-hydroxyquinoline derivatives nitroxoline and clioquinol are used to treat microbial infections; however, these drugs are underused, being available in few countries or limited to topical use. After years of few advances, in the last two decades, the potent activity of clioquinol and nitroxoline against several targets and the privileged structure of 8-hydroxyquinoline nucleus have prompted an increased interest in the design of novel antimicrobial, anticancer, and anti-Alzheimer agents based on this class. Herein, we discuss the current development and antimicrobial structure–activity relationships of this class in the perspective of using the 8-hydroxyquinoline nucleus for the search for novel antimicrobial agents. Furthermore, the most investigated molecular targets concerning 8-hydroxyquinoline derivatives are explored in the final section.

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新型抗菌 8-羟基喹啉类药物：当前发展、构效关系和展望

由于新的微生物菌株的出现耐药性，寻找新的抗菌剂势在必行。在这种情况下，重新审视 8-羟基喹啉等已知类别可能是发现新药物的有趣策略。8-羟基喹啉衍生物硝唑啉和氯碘羟喹用于治疗微生物感染；然而，这些药物未得到充分利用，在少数国家可用或仅限于局部使用。经过多年的进展，在过去的二十年中，氯碘羟喹和硝唑啉对几个靶点的有效活性以及 8-羟基喹啉核的特殊结构促使人们对设计新型抗菌、抗癌和抗阿尔茨海默病药物的兴趣增加基于这个类。在此处，我们从使用 8-羟基喹啉核寻找新型抗菌剂的角度讨论了该类别的当前发展和抗菌结构-活性关系。此外，最后一节探讨了研究最多的关于 8-羟基喹啉衍生物的分子靶点。