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Synthesis of Degraded Limonoid Analogs as New Antibacterial Scaffolds against Staphylococcus aureus.
Antibiotics ( IF 4.8 ) Pub Date : 2020-08-06 , DOI: 10.3390/antibiotics9080488
Marta Ferrera-Suanzes 1 , Victoria Prieto 2 , Antonio J Medina-Olivera 1 , José Manuel Botubol-Ares 1 , Fátima Galán-Sánchez 2, 3 , Manuel A Rodríguez-Iglesias 2, 3 , Rosario Hernández-Galán 1, 3 , María Jesús Durán-Peña 1
Affiliation  

Staphylococcus aureus and methicillin-resistant Staphylococcus aureus (MRSA) have become serious infections in humans and ruminants. S. aureus strains are showing rapid changes to develop resistance in traditional antibiotic-containing systems. In the continuous fierce fight against the emergent multi-drug resistant bacterial strains, straightforward and scalable synthetic procedures to produce new active molecules are in demand. Analysis of molecular properties points to degraded limonoids as promising candidates. In this article, we report a simple synthetic approach to obtain degraded limonoid analogs as scaffolds for new antibacterial molecules. The minimum inhibitory concentrations against S. aureus were evaluated for the stereoisomer mixtures by the broth microdilution method. Analysis of results showed that the acetylated derivatives were the most active of them all.

中文翻译:

降解柠檬苦素类似物作为抗金黄色葡萄球菌的新型抗菌支架。

金黄色葡萄球菌和耐甲氧西林的 黄色葡萄球菌(MRSA)已成为人类和反刍动物的严重感染。在传统的含抗生素系统中,金黄色葡萄球菌菌株显示出迅速的变化以产生抗药性。在与新兴的耐多药细菌菌株的激烈竞争中,需要直接且可扩展的合成程序来生产新的活性分子。分子特性分析表明降解的柠檬苦素类化合物是有前途的候选物。在本文中,我们报告了一种简单的合成方法,以获取降解的柠檬苦素类似物作为新型抗菌分子的支架。对金黄色葡萄球菌的最低抑制浓度通过肉汤微量稀释法评估立体异构体混合物的浓度。结果分析表明,乙酰化衍生物是所有活性最高的。
更新日期:2020-08-06
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