With the widespread use and sometimes even abuse of antibiotics, the problem of bacterial resistance to antibiotics has become very serious, and it is posing a great threat to global health. Therefore, development of new antibiotics is imperative. Triazoles are five-membered, nitrogen-containing aromatic heterocyclic scaffolds, with two isomeric forms, i.e. 1,2,3-triazole and 1,2,4-triazole. Triazole-containing compounds have a wide range of biological activities such as antibacterial, antifungal, anticancer, antioxidant, antitubercular, antimalarial, anti-HIV, anticonvulsant, anti-inflammatory, antiulcer, analgesic, and etc. The bioactivities and the diversity of triazole-containing drugs have attracted wide interest in these heterocycles. Various antibiotic triazole hybrids have been developed, and most of which have shown potent antimicrobial activities. In this review, we summarized the recent advances in triazole hybrids as potential antibacterial agents and their structure-activity relationships (SARs). The information gained through SAR studies will provide further insights into the development of new triazole antimicrobials.

随着抗生素的广泛使用甚至滥用，细菌对抗生素的耐药性问题变得非常严重，对全球健康构成巨大威胁。因此，开发新型抗生素势在必行。三唑类化合物是五元含氮芳香杂环骨架，具有两种异构形式，即1,2,3-三唑和1,2,4-三唑。三唑类化合物具有抗菌、抗真菌、抗癌、抗氧化、抗结核、抗疟、抗HIV、抗惊厥、抗炎、抗溃疡、镇痛等多种生物活性。含有药物的这些杂环引起了广泛的兴趣。已经开发出多种抗生素三唑杂合体，其中大多数显示出有效的抗菌活性。在这篇综述中，我们总结了三唑杂化物作为潜在抗菌剂的最新进展及其构效关系（SAR）。通过 SAR 研究获得的信息将为新型三唑类抗菌药物的开发提供进一步的见解。