Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, West Wenhua Road, 44, Jinan, 250012, P.R. China.
ChemMedChem. 2020 Oct 19;15(20):1875-1886. doi: 10.1002/cmdc.202000378. Epub 2020 Sep 11.
Multidrug-resistant bacterial infections have become an important cause of clinical death in the twenty-first century. Much effort has been made to overcome this challenge. The discovery of novel antimicrobial compounds, as well as the rational use of antibacterial drugs with different structure types and mechanisms, is helping to deal with bacterial resistance. Currently, pyrimidine-containing agents are the major areas of new antibacterial drug discovery. Given their good activities and diverse mechanisms of action, many pyrimidine-containing heterocyclic compounds have become the focus of interest for many scientists. In addition, pyrimidine structure is an important part of many endogenous substances, which is an advantage that allows pyrimidine derivatives to interact with genetic materials, enzymes and other biopolymeric substances in the cell. Scientists have focused on the discovery and structural optimization of pyrimidine derivatives, which has resulted in the discovery of many novel pyrimidine derivatives with intriguing profiles. Herein we summarize the therapeutic potentials of pyrimidine compounds that are promising for antimicrobial applications over the last decade. In particular, the relationships between the structures of modified pyrimidines and their antimicrobial activity are systematically discussed.
耐多药细菌感染已成为 21 世纪临床死亡的重要原因。人们付出了大量努力来克服这一挑战。新型抗菌化合物的发现,以及不同结构类型和作用机制的抗菌药物的合理使用,有助于应对细菌耐药性。目前,含嘧啶的药物是新抗菌药物发现的主要领域。鉴于其良好的活性和多样化的作用机制,许多含嘧啶的杂环化合物已成为许多科学家关注的焦点。此外,嘧啶结构是许多内源性物质的重要组成部分,这一优势使嘧啶衍生物能够与细胞内的遗传物质、酶和其他生物聚合物质相互作用。科学家们专注于嘧啶衍生物的发现和结构优化,这导致了许多具有有趣特性的新型嘧啶衍生物的发现。本文总结了过去十年中具有抗菌应用前景的嘧啶类化合物的治疗潜力。特别地,系统讨论了修饰嘧啶的结构与其抗菌活性之间的关系。