| 含有取代吲哚满二酮-1-乙基的加替沙星衍生物的合成与抗结核作用研究 |
| |
| 引用本文： | 万志龙,刘明亮,冯连顺,王博,郑旭东,郭慧元.含有取代吲哚满二酮-1-乙基的加替沙星衍生物的合成与抗结核作用研究[J].中国抗生素杂志,2011,36(1). |
| |
| 作者姓名： | 万志龙 刘明亮 冯连顺 王博 郑旭东 郭慧元 |
| |
| 作者单位： | 中国医学科学院北京协和医学院医药生物技术研究所,北京,100050 |
| |
| 基金项目： | “重大新药创制”科技重大专项(2009ZX09301-003);“艾滋病和病毒性肝炎等重大传染病防治”科技重大专项“结核病靶标研究”(2008ZX10003-006) |
| |
| 摘 要： | 目的寻找具有优秀活性的喹诺酮类抗结核药物。方法设计合成脂溶性更大的含有取代吲哚满二酮-1-乙基的加替沙星衍生物,测定其体外抗分枝杆菌活性。结果共合成了14个新化合物,其结构经1H-NMR、MS和HRMS确证。目标物普遍具有良好的抗分枝杆菌活性(MIC为1.56~6.25μg/mL),但均弱于其母药加替沙星。其中,化合物3h对草分枝杆菌CMCC93201和耻垢分枝杆菌CMCC93202的活性分别是利福平的4倍和2倍。结论脂溶性并非决定喹诺酮类化合物抗分枝杆菌活性的唯一因素。
|
| 关 键 词： | 加替沙星衍生物 合成 抗分枝杆菌活性 |
Synthesis and in vitro antimycobacterial activity of gatifloxacin ethylene isatin derivatives |
| |
| Wan Zhi-long,Liu Ming-liang,Feng Lian-shun,Wang Bo,Zheng Xu-dong,Guo Hui-yuan.Synthesis and in vitro antimycobacterial activity of gatifloxacin ethylene isatin derivatives[J].Chinese Journal of Antibiotics,2011,36(1). |
| |
| Authors: | Wan Zhi-long Liu Ming-liang Feng Lian-shun Wang Bo Zheng Xu-dong Guo Hui-yuan |
| |
| Institution: | Wan Zhi-long,Liu Ming-liang,Feng Lian-shun,Wang Bo,Zheng Xu-dong and Guo Hui-yuan(Institute of Medicinal Biotechnology,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050) |
| |
| Abstract: | Objective To find new anti-tuberculosis agents of quinolones with high activity. Methods A series of novel gatifloxacin ethylene isatin derivatives possessing more lipophilicity were designed, synthesized and evaluated for their in vitro activity against mycobacteria. Results Fourteen new compounds were obtained and characterized by 1H-NMR, MS and HRMS. These derivatives have considerable activity against the tested two strains (MIC1.56~6.25μg/mL), although less active than the parent drug gatifloxacin. Compound 3h was 4-fold and 2-fold more potent than rifampin against M. phlei CMCC 93201 and M. smegmatis CMCC 93202, respectively. Conclusion The lipophilicity of the new compounds is not the sole parameter affecting antimycobacterial activity. |
| |
| Keywords: | Gatifloxacin derivatives Synthesis Antimycobacterial activity |
| 本文献已被 CNKI 万方数据 等数据库收录！ |
|
