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Cover Feature: Design and Synthesis of Pyrophosphate‐Targeting Vancomycin Derivatives for Combating Vancomycin‐Resistant Enterococci (ChemMedChem 16/2018)
ChemMedChem ( IF 3.4 ) Pub Date : 2018-08-19 , DOI: 10.1002/cmdc.201800522
Dongliang Guan 1, 2 , Feifei Chen 1 , Faridoon 1, 2 , Junjie Liu 1, 3 , Jian Li 1, 2 , Lefu Lan 1, 2, 4 , Wei Huang 1, 2, 5
Affiliation  

The Cover Feature shows a series of new vancomycin analogues carrying a metal‐chelating structure rendering enhanced interaction with the pyrophosphate moiety on the bacterial membrane. Vancomycin‐resistant bacteria develop a mutation of d‐Ala‐d‐Ala to d‐Ala‐d‐Lac on their cell wall to escape vancomycin treatment by a decrease in binding affinity. A pyrophosphate‐targeting strategy for chemical modification of vancomycin enables improved binding to bacteria and compensates the loss of inteaction caused by the mutation. These new vancomycin derivatives demonstrated excellent antibacterial activity against vancomycin‐resistant Enterococcus. More information can be found in the Full Paper by Lefu Lan, Wei Huang et al. on page 1644 in Issue 16, 2018 (DOI: 10.1002/cmdc.201800252).
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中文翻译:

封面特色:用于抗万古霉素抗肠球菌的焦磷酸靶向万古霉素衍生物的设计与合成(ChemMedChem 16/2018)

Cover Feature展示了一系列新的万古霉素类似物,它们具有金属螯合结构,从而增强了与细菌膜上焦磷酸盐部分的相互作用。耐万古霉素的细菌的发展的突变d -Ala- d -Ala到d -Ala- d在它们的细胞壁-LAC逃脱通过在结合亲和力的减少万古霉素治疗。针对万古霉素进行化学修饰的焦磷酸靶向策略可改善与细菌的结合并补偿由突变引起的整合缺失。这些新的万古霉素衍生物对耐万古霉素的肠球菌具有出色的抗菌活性。可以在Lefu Lan,Wei Huang等人的论文全文中找到更多信息。上2018年第16期第1644页(DOI:10.1002 / cmdc.201800252)。
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更新日期:2018-08-19
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