Synthesis and In Vitro Antimycobacterial and Antibacterial Activity of 8-OMe Ciprofloxacin-Hydrozone/Azole Hybrids

被引：32
作者：
Xu, Zhi [1 ,2 ,3 ]
Zhang, Shu [4 ]
Feng, Lian-Shun [2 ,3 ]
Li, Xiao-Ning [2 ,3 ]
Huang, Guo-Cheng [1 ,2 ,3 ]
Chai, Yun [2 ,3 ]
Lv, Zao-Sheng [1 ]
Guo, Hui-Yuan [2 ,3 ]
Liu, Ming-Liang [2 ,3 ]
机构：
[1] Wuhan Univ Sci & Technol, Key Lab Hubei Prov Coal Convers & New Carbon Mat, Wuhan 430081, Hubei, Peoples R China
[2] Chinese Acad Med Sci, Inst Med Biotechnol, Beijing 100050, Peoples R China
[3] Peking Union Med Coll, Beijing 100050, Peoples R China
[4] Pony Testing Int Grp Wuhan, Wuhan 430000, Hubei, Peoples R China
来源：
MOLECULES | 2017年 / 22卷 / 07期
关键词：
8-OMe ciprofloxacin; hybrids; synthesis; antimycobacterial; antibacterial; DERIVATIVES; QUINOLONE; TUBERCULOSIS; FLUOROQUINOLONES; DESIGN; SERIES;
D O I：
10.3390/molecules22071171
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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 7) show potency against Mycobacterium tuberculosis (MTB) H(37)Rv (minimum inhibitory concentration (MIC): <0.5 mu M), 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 mu g/mL), and most Gram-negative strains (MIC: <0.03-4 mu g/mL).
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页数：14
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