| 氟康唑新衍生物的合成与体外抗真菌活性研究 |
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| 引用本文： | 谭文娟,刘兴东,杨帆,胡馨月,白国静,朱伟伟,孟庆国.氟康唑新衍生物的合成与体外抗真菌活性研究[J].烟台大学学报(自然科学与工程版),2013(4):271-275. |
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| 作者姓名： | 谭文娟 刘兴东 杨帆 胡馨月 白国静 朱伟伟 孟庆国 |
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| 作者单位： | 烟台大学药学院,山东烟台264005 |
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| 基金项目： | 国家自然科学基金资助项目（81072534）. |
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| 摘 要： | 基于前期计算机辅助药物研究结果,结合Lipinski类药规则,保留了氟康唑的2,4-二氟苯基、叔醇羟基和一个三唑环,合成了8个C-3连接尿嘧啶侧链的氟康唑新衍生物,并测定了其体外抗真菌活性.新衍生物结构经1H NMR、MS确证,初步体外抗真菌活性试验表明,化合物3b对新生隐球菌表现出一定的抗真菌活性.
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| 关 键 词： | 氟康唑 衍生物 合成 体外抗真菌活性 |
Synthesis and in vitro Antifungal Activity of Novel Fluconazole Derivatives |
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| TAN Wen-juan,LIU Xing-dong,YANG Fan,HU Xin-yue,BAI Guo-jing,ZHU Wei-wei,MENG Qing-guo.Synthesis and in vitro Antifungal Activity of Novel Fluconazole Derivatives[J].Journal of Yantai University(Natural Science and Engineering edirion),2013(4):271-275. |
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| Authors: | TAN Wen-juan LIU Xing-dong YANG Fan HU Xin-yue BAI Guo-jing ZHU Wei-wei MENG Qing-guo |
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| Institution: | (School of Pharmacy, Yantai University, Yantai 2640a5 ,China) |
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| Abstract: | Based on our previous computer-aided drug design results and Lipinski＇s rules, eight new fluconazole derivatives containing uracil linked to C-3 are synthesized by retaining the difluorophenyl group, the hydroxyl group and the triazole ring of fluconazole and their in vitro antifungal activities are determined. The structures of flucon- azole derivatives are confirmed by X n NMR and MS. Preliminary in vitro antifungal activities bioassay shows that compound 3b exhibits moderate in vitro antifungal activities against C. neo. |
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| Keywords: | fluconazole derivative synthesis in vitro antifungal activity |
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