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| 1-(1H-1,2,4-三唑-1-基)-2-(2,4-二氟苯基)-3-(N-环丙基-N-取代氨基)-2-丙醇的合成及其抗真菌活性 |
| 路小娟1,赵庆杰1,叶光明2,邹燕1,胡宏岗1,徐建明1,吴秋业1* |
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| (1. 第二军医大学药学院有机化学教研室,上海 200433;2. 解放军第101医院药剂科,无锡 214044) |
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| 摘要: |
| 目的:研究具有环丙基结构的三唑醇类化合物的抗真菌活性。方法:设计合成了10个三唑醇类新化合物,其结构通过1HNMR、MS和元素分析验证,选择8种真菌为实验菌株,进行体外抑菌活性测试。结果:目标化合物对8种真菌特别是深部真菌均有一定的抑制活性,部分化合物对白念珠菌的MIC80值<0.125 μg/ml,是氟康唑活性的4倍以上。结论:引入环丙基和烷基侧链的目标化合物都具有抗真菌活性,随着烷基侧链增长,目标化合物的活性降低。 |
| 关键词: 合成 三唑醇类 环丙基 抗真菌药 |
| DOI：10.3724/SP.J.1008.2008.01380 |
| 投稿时间：2008-06-11修订日期：2008-09-01 |
| 基金项目:国家自然科学基金(20772153),第二军医大学青年启动基金. |
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| Synthesis of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluoro-phenyl)-3-(N-cyclopropyl-N-substituted amino)-2-propanols and its antifungal activity |
| LU Xiao-juan1,ZHAO Qing-jie1,YE Guang-ming2,ZOU Yan1,HU Hong-gang1,XU Jian-ming1,WU Qiu-ye1* |
| (1.Department of Organic Chemistry,School of Pharmacy,Second Military Medical University,Shanghai 200433,China;2.Department of Pharmacy,No.101 Hospital of PLA,Wuxi 214044) |
| Abstract: |
| Objective:To study the antifungal activity of triazole alcohols by introduction of cyclopropyl as side chain. Methods: Ten title compounds were synthesized and characterized by 1HNMR,MS spectra and element analysis. The MICs of the compounds were determined by in vitro test in 8 fungus strains. Results: The title compounds exhibited potent antifungal activities against 8 strains,especially for the deep infection ones. Some compounds had MIC80 values less than 0.125 μg·ml-1 against Candida albicans,showing an activity 4 time higher than that of fluconzole.Conclusion: The title compounds with cyclopropyl and alky substituents have antifungal activities,and the antifungal activity decreases as the alkyl side chains getting longer. |
| Key words: synthesis triazole cyclopropyl antifungal agents |
