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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 |
| 赵庆杰1,胡宏岗1,叶光明2,俞世冲1,邹燕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9个三唑醇类新化合物,所有目标化合物结构都通过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比较强的抑制活性,所有目标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,与伊曲康唑活性相当。结论:1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluoro-phenyl)-3-\[N-cyclopropyl-N-(3,4-dichlorobenzyl)amino\]-propanol(化合物6f)的活性比较好,有进一步研究开发的价值。 |
| 关键词: 药物化学 三唑类 环丙基 体外抗真菌活性 |
| DOI：10.3724/SP.J.1008.2009.0198 |
| 投稿时间：2008-09-02修订日期：2008-11-18 |
| 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 test of its antifungal activity |
| ZHAO Qing-jie1,HU Hong-gang1,YE Guang-ming2,YU Shi-chong1,ZOU Yan1,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: Nine title compounds were synthesized and characterized by 1HNMR,MS spectra and element analysis.Eight fungi were used for in vitro anti-fungal test.Results: All of the title compounds showed antifungal activities of different extents,especially to the deep infection ones,and they had a MIC value < 0.125 μg/ml against Candida albicans,showing an anti-fungal activity 4 times higher than that of fluconzole and similar to that of totraconazaole.Conclusion: 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluoro-phenyl)-3-\[N-cyclopropyl-N-(3,4-dichlorobenzyl) amino\]-2-propanols(6f) has a better activity ratio and is worth further studying. |
| Key words: medicinal chemistry triazoles cyclopropyl antifungal activity in virtro |
