Song Di, Ma Shutao
Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan, 250012, P.R. China.
ChemMedChem. 2016 Apr 5;11(7):646-59. doi: 10.1002/cmdc.201600041. Epub 2016 Mar 10.
Clinically significant antibiotic resistance is one of the greatest challenges of the twenty-first century. However, new antibacterial agents are currently being developed at a much slower pace than our growing need for such drugs. Given their diverse biological activities and clinical applications, many bioactive heterocyclic compounds containing a benzimidazole nucleus have been the focus of interest for many researchers. The benzimidazole nucleus is a structural isostere of naturally occurring nucleotides. This advantage allows benzimidazoles to readily interact with the various biopolymers found in living systems. In view of this situation, much attention has been given to the exploration of benzimidazole-based antibacterial agents, leading to the discovery of many new chemical entities with intriguing profiles. In this minireview we summarize novel benzimidazole derivatives active against various bacterial strains. In particular, we outline the relationship between the structures of variously modified benzimidazoles and their antibacterial activity.
具有临床意义的抗生素耐药性是21世纪最大的挑战之一。然而，目前新型抗菌药物的研发速度远远跟不上我们对这类药物日益增长的需求。鉴于其多样的生物活性和临床应用，许多含有苯并咪唑核的生物活性杂环化合物已成为众多研究人员关注的焦点。苯并咪唑核是天然存在的核苷酸的结构类似物。这一优势使苯并咪唑能够很容易地与生物系统中发现的各种生物聚合物相互作用。鉴于这种情况，人们对基于苯并咪唑的抗菌剂的探索给予了高度关注，从而发现了许多具有有趣特性的新化学实体。在这篇综述中，我们总结了对各种细菌菌株具有活性的新型苯并咪唑衍生物。特别是，我们概述了各种修饰苯并咪唑的结构与其抗菌活性之间的关系。
