| 含硫的三唑类化合物的合成及抗真菌活性研究 |
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| 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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| 作者姓名： | 张治强 付奔 王保刚 张超 廖万清 潘炜华 郭忠武 |
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| 作者单位： | 第二军医大学药学院有机化学教研室, 上海 200433,第二军医大学药学院有机化学教研室, 上海 200433,第二军医大学药学院有机化学教研室, 上海 200433,第二军医大学附属长征医院皮肤科, 上海 200003,第二军医大学附属长征医院皮肤科, 上海 200003,第二军医大学附属长征医院皮肤科, 上海 200003,第二军医大学药学院有机化学教研室, 上海 200433 |
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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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| 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1 H 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。
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| 关 键 词： | 三唑 合成 抗真菌活性 |
| 收稿时间： | 1/7/2016 12:00:00 AM |
| 修稿时间： | 2016/3/17 0:00:00 |
Synthesis and antifungal activities of novel triazole derivatives containing sulfur atoms |
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| ZHANG Zhiqiang,FU Ben,WANG Baogang,ZHANG Chao,LIAO Wanqing,PAN Weihua and GUO Zhongwu.Synthesis and antifungal activities of novel triazole derivatives containing sulfur atoms[J].The Journal of Pharmaceutical Practice,2016,34(4):334-337. |
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| Authors: | ZHANG Zhiqiang FU Ben WANG Baogang ZHANG Chao LIAO Wanqing PAN Weihua and GUO Zhongwu |
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| Institution: | Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China,Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China,Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China,Department of Dermatology, Changzheng Hospital Affiliated to Second Military Medical University, Shanghai 200003, China,Department of Dermatology, Changzheng Hospital Affiliated to Second Military Medical University, Shanghai 200003, China,Department of Dermatology, Changzheng Hospital Affiliated to Second Military Medical University, Shanghai 200003, China and Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China |
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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. |
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| Keywords: | triazole synthesis antifungal activities |
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