| 氟康唑衍生物的设计与合成 |
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| 引用本文： | 高一军,王楠,李文娟,张雷,柴晓云,王文艳,孙海军,毕毅,吴秋业,孟庆国. 氟康唑衍生物的设计与合成[J]. 中国新药杂志, 2012, 0(6): 681-685,700 |
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| 作者姓名： | 高一军 王楠 李文娟 张雷 柴晓云 王文艳 孙海军 毕毅 吴秋业 孟庆国 |
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| 作者单位： | 烟台大学药学院;第二军医大学药学院 |
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| 基金项目： | 国家自然科学基金(81072534) |
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| 摘 要： | 目的:设计并合成氟康唑衍生物。方法:基于前期计算机辅助药物设计结果,以氟康唑为先导化合物,保留2,4-二氟苯基、叔醇羟基和一个三氮唑,在3位C上引入不同的取代氨基,设计经取代,酯化,溴代,缩合,皂化,缩合6步反应合成目标化合物。结果:合成了13个新化合物,结构经1H-NMR,MS确证。结论:合成路线设计合理,目标化合物结构正确,可供下一步的药理研究。
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| 关 键 词： | 氟康唑 衍生物 设计 合成 |
Design and synthesis of fluconazole derivatives |
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| GAO Yi-jun,WANG Nan,LI Wen-juan,ZHANG Lei,CHAI Xiao-yun,WANG Wen-yan,SUN Hai-jun,BI Yi,WU Qiu-ye,MENG Qing-guo. Design and synthesis of fluconazole derivatives[J]. Chinese Journal of New Drugs, 2012, 0(6): 681-685,700 |
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| Authors: | GAO Yi-jun WANG Nan LI Wen-juan ZHANG Lei CHAI Xiao-yun WANG Wen-yan SUN Hai-jun BI Yi WU Qiu-ye MENG Qing-guo |
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| Affiliation: | 1(1 School of Pharmacy,Yantai University,Yantai 264005,China;2 School of Pharmacy, Second Military Medical University,Shanghai 200433,China) |
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| Abstract: | Objective: To design and synthesize fluconazole derivatives.Methods: Based on the previous result of computer-aided drug design,we systematically altered the structure of fluconazole according to the structure-activity relationships of the azoles in antifungal compounds and synthesized target compounds in six steps.Results: Thirteen new compounds were synthesized.The structures were confirmed by 1H-NMR and MS.Conclusion: The design of synthetic route is reasonable.Target compounds are correct and can be used for further study of pharmacological activities. |
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| Keywords: | fluconazole derivative design synthesis |
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