| 含硫的三唑类化合物的合成及抗真菌活性研究 |
| 投稿时间：2016-01-07 修订日期：2016-03-17 点此下载全文 |
| 引用本文：张治强,付奔,王保刚,张超,廖万清,潘炜华,郭忠武.含硫的三唑类化合物的合成及抗真菌活性研究[J].药学实践杂志,2016,34(4):334~337 |
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| 基金项目:国家自然科学基金（20972188），上海科委重点攻关课题（09dZ1976700，10dZ2220100） |
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| 中文摘要:目的 设计合成含有二硫代甲酸酯侧链的新型三氮唑类化合物，并研究其体外抗真菌活性。方法 通过与二硫化碳的加成及取代反应合成了9个新型三氮唑类化合物，其结构通过1H NMR和MS确证，并选择8种真菌为实验菌株，对其体外抗真菌活性进行测试。结果 所有化合物对实验菌株均有一定的抗菌活性，尤其对白色念珠菌活性较好，化合物6d对白假丝酵母菌的MIC80值<0.125μg/ml，是伊曲康唑的64倍。结论 引入丙基、硫元素和取代苄基侧链对目标化合物的抗真菌活性影响较大；二硫代甲酸酯结构的引入有利于提高三唑类化合物的体外抗真菌活性。 |
| 中文关键词:三唑 合成 抗真菌活性 |
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| Synthesis and antifungal activities of novel triazole derivatives containing sulfur atoms |
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| Abstract:Objective To design and synthesis novel triazole antifungal derivatives with dithiocarbamates side chain and study the antifungal activities. Methods Nine title compounds were synthesized and characterized by 1H NMR, MS spectra. The in vitro antifungal activities of all the compounds were evaluated against eight human pathogenic fungi. Results The title compounds exhibited strong antifungal activities. Some compounds showed excellent activities against Candida albicans with the MIC80 values less than 0.125 g/ml, 6d was 64 times higher than that of Itraconazole. Conclusion The introduction of the propyl, sulphur and benzyl moiety to the side chain could affect the antifungal activities. |
| keywords:triazole synthesis antifungal activities |
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