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未来的抗生素:天然和功能化的酚类化合物。

Future Antimicrobials: Natural and Functionalized Phenolics.

机构信息

Faculty of Medicine and Biological Sciences, "Ştefan cel Mare" University, 720229 Suceava, Romania.

Faculty of Chemistry, "Alexandru Ioan Cuza" University, 700506 Iasi, Romania.

出版信息

Molecules. 2023 Jan 22;28(3):1114. doi: 10.3390/molecules28031114.

Abstract

With incidence of antimicrobial resistance rising globally, there is a continuous need for development of new antimicrobial molecules. Phenolic compounds having a versatile scaffold that allows for a broad range of chemical additions; they also exhibit potent antimicrobial activities which can be enhanced significantly through functionalization. Synthetic routes such as esterification, phosphorylation, hydroxylation or enzymatic conjugation may increase the antimicrobial activity of compounds and reduce minimal concentrations needed. With potent action mechanisms interfering with bacterial cell wall synthesis, DNA replication or enzyme production, phenolics can target multiple sites in bacteria, leading to a much higher sensitivity of cells towards these natural compounds. The current review summarizes some of the most important knowledge on functionalization of natural phenolic compounds and the effects on their antimicrobial activity.

摘要

随着全球抗菌药物耐药性的上升,人们不断需要开发新的抗菌分子。具有多功能支架的酚类化合物允许进行广泛的化学添加;它们还表现出强大的抗菌活性,通过功能化可以显著增强。酯化、磷酸化、羟化或酶偶联等合成途径可以提高化合物的抗菌活性,并减少所需的最小浓度。由于酚类化合物具有强大的作用机制,可干扰细菌细胞壁合成、DNA 复制或酶产生,因此可以针对细菌中的多个靶位,导致细胞对这些天然化合物的敏感性大大提高。本综述总结了一些关于天然酚类化合物的功能化及其对其抗菌活性影响的重要知识。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a59f/9920704/ab1c17573e4f/molecules-28-01114-g001.jpg

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