Synthetic Optimization and Antibacterial Activity of Novel Benzodioxepine-Biphenyl Amide Derivatives.

IF 1.2 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Acta Chimica Slovenica Pub Date : 2024-08-31 DOI:10.17344/acsi.2024.8784
Shao-Peng Yan, Zhi-Yu Zhu, Qi-Ke Jia, Rui-Ying Ji, Ya-Pin Wang, Dan He, Rong Wang, Yang Zhou
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Abstract

The biosynthesis of fatty acids constitutes a critical metabolic pathway in bacterial organisms. Prior investigations have highlighted the synthesis of antimicrobial compounds anchored in the benzodioxepin scaffold, noted for their pronounced antibacterial properties. Leveraging this foundational knowledge, the current research endeavors to meticulously engineer and synthesize a series of eight innovative benzodioxepin amide-biphenyl derivatives. This achievement was realized through the sophisticated optimization of synthetic methodologies. The scope of this study extends to a rigorous evaluation of the antibacterial prowess and biocompatibility of the aforementioned novel derivatives. Notably, Compound E4 emerged as a supremely potent antimicrobial agent. A detailed elucidation of the crystalline architecture of Compound E4 was conducted, alongside a thorough docking study to explore its interactions with the FabH enzyme.

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新型苯并二氧杂环庚烷-联苯酰胺衍生物的合成优化和抗菌活性。
脂肪酸的生物合成是细菌生物体的一个重要代谢途径。先前的研究突出了以苯并二氧杂环庚烷为支架的抗菌化合物的合成,这些化合物具有显著的抗菌特性。利用这些基础知识,目前的研究致力于精心设计和合成一系列八种创新的苯并二氧杂环庚烷酰胺联苯衍生物。这一成果是通过复杂的合成方法优化实现的。本研究的范围扩展到对上述新型衍生物的抗菌能力和生物相容性进行严格评估。值得注意的是,化合物 E4 是一种极其有效的抗菌剂。研究人员详细阐明了化合物 E4 的晶体结构,并进行了深入的对接研究,以探索其与 FabH 酶的相互作用。
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来源期刊
Acta Chimica Slovenica
Acta Chimica Slovenica 化学-化学综合
CiteScore
2.50
自引率
25.00%
发文量
80
审稿时长
1.0 months
期刊介绍: Is an international, peer-reviewed and Open Access journal. It provides a forum for the publication of original scientific research in all fields of chemistry and closely related areas. Reviews, feature, scientific and technical articles, and short communications are welcome.
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