化学
金黄色葡萄球菌
抗菌活性
耐甲氧西林金黄色葡萄球菌
腙
取代基
氧氟沙星
抗菌剂
生物膜
微生物学
抗生素
组合化学
立体化学
细菌
有机化学
生物化学
环丙沙星
生物
遗传学
作者
Xueer Lu,Qian Zhang,Yingying Xu,Jun Lü,Wenjian Tang,Jing Zhang
出处
期刊:RSC Advances
[The Royal Society of Chemistry]
日期:2020-01-01
卷期号:10 (30): 17854-17861
被引量:13
摘要
Carbonyl cyanide m-chlorophenylhydrazone (CCCP), as a protonophore, in combination with antibiotics exhibited potentiating antibacterial activity. To improve CCCP's potency and toxicity, a series of aromatic hydrazones were synthesized and their antimicrobial activity was evaluated; amongst them, compounds 2e and 2j with a strong para-electron-withdrawing substituent (-NO2 and -CF3) at the phenyl ring had the lowest MICs against both S. aureus and methicillin resistant Staphylococcus aureus (1.56 and 1.56 μM, respectively). Some compounds in combination with antibiotics exhibited potentiate Gram-positive antibacterial activity; compound 2e was found to display unaided or synergistic efficacy against MRSA. In particular, when compound 2e is combined with ofloxacin, it has a good synergistic effect against MRSA. Moreover, electron microscopy revealed that compound 2e inhibits biofilm formation and effectively eradicates preformed biofilm. MTT assay showed that compound 2e displays as low toxicity as CCCP. Overall, our data showed that the aromatic hydrazone is a promising scaffold for anti-staphylococcal drug development.
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