八肽菌素C4的合成及其对新德里金属β-内酰胺酶-1（NDM-1）和耐多粘菌素细菌的生物学特性分析
Synthesis of octapeptin C4 and biological profiling against NDM-1 and polymyxin-resistant bacteria.
作者信息
Becker Bernd, Butler Mark S, Hansford Karl A, Gallardo-Godoy Alejandra, Elliott Alysha G, Huang Johnny X, Edwards David J, Blaskovich Mark A T, Cooper Matthew A
机构信息
Institute of Molecular Bioscience, University of Queensland, Brisbane 4072, Australia.
Institute of Molecular Bioscience, University of Queensland, Brisbane 4072, Australia.
出版信息
Bioorg Med Chem Lett. 2017 Jun 1;27(11):2407-2409. doi: 10.1016/j.bmcl.2017.04.027. Epub 2017 Apr 12.
Abstract
The first synthesis of octapeptin C4 was achieved using a combination of solid phase synthesis and off-resin cyclisation. Octapeptin C4 displayed antibiotic activity against multi-drug resistant, NDM-1 and polymyxin-resistant Gram-negative bacteria, with moderate activity against Staphylococcus aureus. The linear analogue of octapeptin C4 was also prepared, which showed reduced activity.
摘要
八肽菌素C4的首次合成是通过固相合成和脱树脂环化相结合的方法实现的。八肽菌素C4对多重耐药、NDM-1和耐多粘菌素的革兰氏阴性菌具有抗菌活性，对金黄色葡萄球菌具有中等活性。还制备了八肽菌素C4的线性类似物，其活性有所降低。
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