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| 1-(1H-1, 2,4-三唑-1-基)-2-(2, 4-二氟苯基)-3-取代-2-丙醇类化合物的合成及抗真菌活性 |
| 周宇1,俞世冲2,王保刚2,闫永正2,吴秋业2* |
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| (1. 解放军82医院药剂科,淮安 223001;2. 第二军医大学药学院有机化学教研室,上海 200433) |
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| 摘要: |
| 目的研究具有正丁基和三氮唑侧链结构的三唑醇类化合物的抗真菌活性。方法设计合成了16个1-(1H-1, 2, 4-三唑-1-基)-2-(2, 4-二氟苯基)-3-取代-2-丙醇类化合物,其结构都经过 1HNMR和LC-MS确证。选择8种临床常见的真菌为实验菌株,进行体外抑菌活性测试。结果初步的体外抗真菌测试结果表明,所合成的化合物都有一定的抗真菌活性,其中化合物7b、7d、7e和7i对除薰烟曲霉菌外7种菌株的抑菌活性优于对照药氟康唑,与伊曲康唑相当。结论引入正丁基和三氮唑侧链的目标化合物都具有一定的抗真菌活 |
| 关键词: 合成 三唑类 抗真菌药 |
| DOI：10.3724/SP.J.1008.2011.0754 |
| 投稿时间：2011-03-04修订日期：2011-05-25 |
| 基金项目:国家自然科学基金 |
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| Synthesis and antifungal activity of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanol |
| ZHOU Yu1,YU Shi-chong2,WANG Bao-gang2,YAN Yong-zheng2,WU Qiu-ye2* |
| (1. Department of Pharmacy, No. 82 Hospital of PLA, Huaian 223001, Jiangsu, China;2. Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China) |
| Abstract: |
| Objective: To study the antifungal activity of triazole alcohols by introduction of n-butyl and triazole as side chain. Methods: sixteen 1-(1H-1, 2, 4-Triazole-1-yl)-2-(2, 4-Difluorophenyl)-3-Substituted-2-Propanol were synthesized and characterized by 1H NMR and LC-MS．The MICs of the compounds were determined by in vitro test in eight human pathogenic fungi．Results: The title compounds exhibited potent antifungal activities against nearly all fungi tested. Conclusion: The title compounds with n-butyl and triazole side chain have antifungal activities. |
| Key words: synthesis triazole antifungal activity |
