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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Semisynthesis and biological evaluation of amidochelocardin derivatives as broad-spectrum antibiotics
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Semisynthesis and biological evaluation of amidochelocardin derivatives as broad-spectrum antibiotics

机译：酰胺的半合成与生物学评价衍生物作为广谱抗生素的衍生物

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To address the global challenge of emerging antimicrobial resistance, the hitherto most successful strategy to new antibiotics has been the optimization of validated natural products: most of these efforts rely on semisynthesis. Herein, we report the semisynthetic modification of amidochelocardin, an atypical tetracycline obtained via genetic engineering of the chelocardin producer strain. We report modifications at C4, C7, C10 and C11 by the application of methylation, acylation, electrophilic substitution, and oxidative C-C coupling reactions. The antibacterial activity of the reaction products was tested against a panel of Gram-positive and Gram-negative pathogens. The emerging structure-activity relationships (SARs) revealed that positions C7 and C10 are favorable anchor points for the semisynthesis of optimized derivatives. The observed SAR was different from that known for tetracyclines, which underlines the pronounced differences between the two compound classes. (C) 2019 Elsevier Masson SAS. All rights reserved.
机译：为解决新兴抗菌抗性的全球挑战，迄今为止对新抗生素的最成功的策略一直是经过验证的天然产品的优化：大多数这些努力依赖半合成。在此，我们报告了通过Chelocardin生产商菌株的基因工程获得的非典型四环素的半合成改性。我们通过施用甲基化，酰化，亲电子取代和氧化C-C偶联反应来报告C4，C7，C10和C11的修饰。测试反应产物的抗菌活性对革兰氏阳性和革兰氏阴性病原体的面板进行了测试。新兴结构 - 活动关系（SARS）揭示了位置C7和C10是优化衍生物的半合成的有利锚点。观察到的SAR与四环素中已知的不同，这强调了两种复合类别之间的显着差异。 （c）2019年Elsevier Masson SAS。版权所有。

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