Novel benzyl phenyl sulfide derivatives as antibacterial agents against methicillin-resistant Staphylococcus aureus
Novel benzyl phenyl sulfide derivatives as antibacterial agents against methicillin-resistant Staphylococcus aureus
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新型苯甲基苯硫醚衍生物作为耐甲氧西林金黄色葡萄球菌的抗菌剂
DOI：
10.1038/s41429-019-0257-x
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发表时间：
2019-11
影响因子：
3.3
通讯作者：
Chen Wei-Min
中科院分区：
文献类型：
--
作者：
Lu Kuo;Chen Qi;Xu Xiao-Fang;Meng Ying;Lin Jing;Chen Wei-Min
耐甲氧西林金黄色葡萄球菌 (MRSA) 感染对人类健康构成重大威胁，因为它对几乎所有类别的抗生素都具有耐药性。迫切需要发现具有新结构、可对抗 MRSA 病原体的新型抗菌剂。本研究设计合成了3个系列的苄基苯基硫醚衍生物，并评价了它们对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具有有效的抗菌活性，最低抑菌浓度为2-64 μg/mL。讨论了构效关系，并表明抗菌活性的机制涉及破坏细菌细胞膜。最后，MTT测定结果表明化合物5f和5h的毒性在细菌和哺乳动物细胞之间具有选择性。
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.
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影响因子：
16
作者：
M. Fauvart;B. Van den Bergh;J. Michiels
通讯作者：
M. Fauvart;B. Van den Bergh;J. Michiels
影响因子：
1.2
作者：
A. Hatano;M. Nishimura;I. Souta
通讯作者：
A. Hatano;M. Nishimura;I. Souta
DOI：
10.1016/s0093-3619(08)70765-2
发表时间：
2008
期刊：
Yearbook of Dermatology and Dermatologic Surgery
影响因子：
--
作者：
B. Thiers
通讯作者：
B. Thiers
药物中含硫支架的合成及其在药物化学中的应用
影响因子：
3.4
作者：
Feng M;Tang B;Liang SH;Jiang X
通讯作者：
Jiang X
影响因子：
6.7
作者：
Geng, Zhi-Zhong;Zhang, Jian-Jun;Chen, Wei-Min
通讯作者：
Chen, Wei-Min