8-甲氧基环丙沙星腙/唑类杂化物的合成及其体外抗分枝杆菌和抗菌活性
Synthesis and In Vitro Antimycobacterial and Antibacterial Activity of 8-OMe Ciprofloxacin-Hydrozone/Azole Hybrids.
作者信息
Xu Zhi, Zhang Shu, Feng Lian-Shun, Li Xiao-Ning, Huang Guo-Cheng, Chai Yun, Lv Zao-Sheng, Guo Hui-Yuan, Liu Ming-Liang
机构信息
Key Laboratory of Hubei Province for Coal Conversion and New Carbon Materials, Wuhan University of Science and Technology, Wuhan 430081, China.
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
出版信息
Molecules. 2017 Jul 13;22(7):1171. doi: 10.3390/molecules22071171.
A series of novel 8-OMe ciprofloxacin (CPFX)-hydrazone/azole hybrids were designed, synthesized, and evaluated for their in vitro biological activities. Our results reveal that all of the hydrozone-containing hybrids (except for ) show potency against (MTB) HRv (minimum inhibitory concentration (MIC): <0.5 μM), which is better than the parent drug CPFX, and comparable to moxifloxacin and isoniazid, some of the tested Gram-positive strains (MIC: 0.06-4 μg/mL), and most Gram-negative strains (MIC: ≤0.03-4 μg/mL).
设计、合成了一系列新型8-甲氧基环丙沙星（CPFX）腙/唑杂合物，并对其体外生物活性进行了评估。我们的结果表明，所有含腙杂合物（除了 ）对结核分枝杆菌（MTB）H37Rv均显示出活性（最低抑菌浓度（MIC）：<0.5 μM），优于母体药物CPFX，与莫西沙星和异烟肼相当，对一些测试的革兰氏阳性菌株（MIC：0.06 - 4 μg/mL）以及大多数革兰氏阴性菌株（MIC：≤0.03 - 4 μg/mL）也有活性。
需注意，原文中部分括号内容缺失具体信息，翻译时保留了原文格式。
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