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单环β-内酰胺类抗生素作为抗菌剂:N-甲基硫代氮杂环丁酮的抗氧化活性。

Monocyclic β-lactams as antibacterial agents: facing antioxidant activity of N-methylthio-azetidinones.

机构信息

Department of Chemistry G. Ciamician, University of Bologna, Via Selmi 2, 40126 Bologna, Italy.

出版信息

Eur J Med Chem. 2013 Feb;60:340-9. doi: 10.1016/j.ejmech.2012.12.024. Epub 2012 Dec 20.

Abstract

A series of N-methylthio-β-lactams with antibacterial activity were thoroughly evaluated as antioxidants. We found that only the presence of a polyphenolic moiety anchored to the β-lactam ring ensured an adequate antioxidant potency. New compounds, efficiently combining in one structure antioxidant and antibacterial activity, may provide a promising basis for the development of new leads useful in adverse clinical conditions such as in cystic fibrosis patients, in whom colonization by MRSA and epithelial damage by chronic pulmonary oxidative stress take place.

摘要

我们评价了一系列具有抗菌活性的 N-甲基硫代-β-内酰胺类化合物作为抗氧化剂的效果。结果发现,只有将多酚基团连接到β-内酰胺环上,才能确保其具有足够的抗氧化能力。这些新化合物将抗氧化和抗菌活性结合在一个结构中,有望为开发新的先导化合物提供有价值的基础,这些先导化合物可用于治疗囊性纤维化患者等不良临床条件下的疾病,此类患者易发生耐甲氧西林金黄色葡萄球菌定植和慢性肺部氧化应激导致的上皮损伤。

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