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首页> 外文期刊>Angewandte Chemie >Ratiometric Fluorescence Detection of Pathogenic Bacteria Resistant to Broad-Spectrum β-Lactam Antibiotics
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Ratiometric Fluorescence Detection of Pathogenic Bacteria Resistant to Broad-Spectrum β-Lactam Antibiotics

机译:广谱β-内酰胺类抗生素耐药细菌的比例荧光检测

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摘要

β-Lactam antibiotics have been the frontline drugs to fight bacterial infections because of their high efficacy and low toxicity ever since they were first discovered in the 1920s. These agents confer their antimicrobial ability by inhibiting transpeptidases, also known as penicillin binding proteins (PBPs), the activity of which is required for bacterial cell wall synthesis. To date, hundreds of β-lactam compounds have been synthesized and evaluated for their antibacterial properties, including derivatives of penicillin, cephalosporin, mono-bactam, and carbapenem. As one of the primary strategies to survive in the presence of these antibiotics, bacterial cells can acquire β-lactamases, a family of highly efficient enzymes that are able to destroy β-lactam structural moieties before they interact with PBPs. Hence, inactivation or inhibition of potential β-lactamases is a key consideration for the treatment of bacterial infections.
机译:自从1920年代首次发现以来,β-内酰胺抗生素一直以来都是对抗细菌感染的前沿药物,因为它们的功效高,毒性低。这些药物通过抑制转肽酶(也称为青霉素结合蛋白(PBPs))来赋予其抗菌能力,其活性是细菌细胞壁合成所必需的。迄今为止,已经合成了数百种β-内酰胺化合物,并对其抗菌性能进行了评估,包括青霉素,头孢菌素,单-bactam和碳青霉烯衍生物。作为在这些抗生素存在下生存的主要策略之一,细菌细胞可以获取β-内酰胺酶,这是一种高效酶,可以在与PBP相互作用之前破坏β-内酰胺结构部分。因此,潜在的β-内酰胺酶的失活或抑制是治疗细菌感染的关键考虑因素。

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