Dipartimento di Chimica e Chimica Industriale, University of Pisa, Via G. Moruzzi, 3, I-56124 Pisa, Italy.
Dipartimento di Scienze Agrarie, Alimentari e Forestali, University of Palermo, Viale delle Scienze, Edificio 4, I-90128 Palermo, Italy.
Molecules. 2020 Nov 4;25(21):5133. doi: 10.3390/molecules25215133.
The rapid growth of serious infections caused by antibiotic resistant bacteria, especially the nosocomial ESKAPE pathogens, has been acknowledged by Governments and scientists and is one of the world's major health problems. Various strategies have been and are currently investigated and developed to reduce and/or delay the bacterial resistance. One of these strategies regards the design and development of antimicrobial hybrids and conjugates. This unprecedented critical review, in which our continuing interest in the synthesis and evaluation of the bioactivity of imidazole derivatives is testified, aims to summarise and comment on the results obtained from the end of the 1900s until February 2020 in studies conducted by numerous international research groups on the synthesis and evaluation of the antibacterial properties of imidazole-based molecular hybrids and conjugates in which the pharmacophoric constituents of these compounds are directly covalently linked or connected through a linker or spacer. In this review, significant attention was paid to summarise the strategies used to overcome the antibiotic resistance of pathogens whose infections are difficult to treat with conventional antibiotics. However, it does not include literature data on the synthesis and evaluation of the bioactivity of hybrids and conjugates in which an imidazole moiety is fused with a carbo- or heterocyclic subunit.
抗生素耐药菌引起的严重感染迅速增长，尤其是医院内的 ESKAPE 病原体，这一问题已引起各国政府和科学家的关注，是世界主要健康问题之一。为了减少和/或延缓细菌耐药性的产生，已经研究并正在开发各种策略。其中一种策略是设计和开发抗菌杂合体和缀合物。本综述前所未有，见证了我们对咪唑衍生物的合成和生物活性评估的持续兴趣，旨在总结和评论自 20 世纪末至 2020 年 2 月期间，许多国际研究小组在合成和评估基于咪唑的分子杂合体和缀合物的抗菌特性方面的研究结果，这些化合物的药效团成分通过连接子或间隔基直接共价连接或连接。在本综述中，我们高度关注总结用于克服难以用传统抗生素治疗感染的病原体的抗生素耐药性的策略。但是，它不包括关于与碳环或杂环亚基融合的咪唑部分的杂合体和缀合物的合成和生物活性评估的文献数据。
