Novel benzyl phenyl sulfide derivatives as antibacterial agents against methicillin-resistant Staphylococcus aureus.,The Journal of Antibiotics

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Novel benzyl phenyl sulfide derivatives as antibacterial agents against methicillin-resistant Staphylococcus aureus.
The Journal of Antibiotics ( IF 2.1 ) Pub Date : 2019-11-14 , DOI: 10.1038/s41429-019-0257-x
Kuo Lu ₁ , Qi Chen ₁ , Xiao-Fang Xu ₁ , Ying Meng ₁ , Jing Lin ₁ , Wei-Min Chen ₁

Affiliation

Methicillin-resistant Staphylococcus aureus (MRSA) infection is a major threat to human health due to its resistance to almost all classes of antibiotics. Discovery of novel antibacterial agents with new structures which combat the pathogens responsible for MRSA is urgent. In this study, three series of benzyl phenyl sulfide derivatives were designed and synthesized, and their antibacterial activity against eleven MRSA strains were evaluated. The results showed that two series of the synthetic compounds (5a-5l and 12p-12u) exhibit potent antibacterial activity against S. aureus and MRSA, with minimum inhibitory concentrations of 2-64 μg/mL. The structure-activity relationships are discussed and the mechanism of the antibacterial activity was shown to involve the destruction of the bacterial cell membrane. Finally, the MTT assay results suggest that the toxicity of compounds 5f and 5h is selective between bacteria and mammalian cells.

中文翻译：

新型苄基苯基硫醚衍生物作为对耐甲氧西林的金黄色葡萄球菌的抗菌剂。

耐甲氧西林金黄色葡萄球菌（MRSA）感染由于对几乎所有类型的抗生素都有抵抗力，因此对人类健康构成重大威胁。迫切需要发现具有抗MRSA病原体新结构的新型抗菌剂。在这项研究中，设计和合成了三个系列的苄基苯基硫醚衍生物，并评估了它们对11种MRSA菌株的抗菌活性。结果表明，两个系列的合成化合物（5a-5l和12p-12u）对金黄色葡萄球菌和MRSA均表现出强大的抗菌活性，最低抑菌浓度为2-64μg/ mL。讨论了结构与活性之间的关系，并显示了抗菌活性的机理涉及细菌细胞膜的破坏。最后，

更新日期：2020-01-16

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