| 没食子酰哌嗪类化合物的合成及抗真菌作用研究 |
| 投稿时间：2019-08-29 修订日期：2019-10-29 点此下载全文 |
| 引用本文：王瀚萱,董家潇,马颖,高越,金永生.没食子酰哌嗪类化合物的合成及抗真菌作用研究[J].药学实践杂志,2020,38(6):506~508,542 |
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| 基金项目:上海市卫计委科研课题（20124057） |
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| 中文摘要:目的 设计合成没食子酰哌嗪衍生物，考察其对耐药真菌的抗菌活性。方法 以三甲氧基没食子酸为原料，在PyBOP/DIEA存在下与哌嗪反应得到中间体，在脱保护后与相应的酸缩合，最后脱甲基得到目标化合物。采用美国国家临床实验室标准委员会（CLSI）推荐方法，将目标化合物对2株临床分离的耐药白色念珠菌株进行体外抗真菌活性试验，进而与氟康唑（8 μg/ml）联用，开展协同抗真菌活性试验。结果 共合成了11个化合物，其中6个化合物表现出优于没食子酸的抗真菌活性。结论 没食子酰哌嗪可以提高没食子酸的抗真菌活性，没食子酸酰结构是重要的药效团，若引入桂皮酸或2,3-二氯苯甲酸可以进一步提高活性。 |
| 中文关键词:没食子酸 抗真菌 协同作用 合成 |
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| Study on synthesis and antifungal activities of galloyl piperazine derivatives |
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| Abstract:Objective To design, synthesize and measure antifungal activities of galloyl piperazine derivatives.Methods Trimethoxyl gallic acid was used as starting material, reacted with piperazine in the presence of PyBOP/DIEA to afford the intermediates. The target compounds were obtained through the reaction with corresponding acids after deprotection gave. The antifungal activities of the target compounds were evaluated by FLC-resistant Candida albican isolated according to the CLSI recommended method.Results 11 target compounds were synthesized and six of them showed more potent antifungal activities than gallic acid.Conclusion Galloyl piperazine derivatives could enhance antifungal activities. Galloyl moiety was an important pharmacophore, which could improve antifungal activities with the introduction of cinnamic acid and 2,3-dichlorobenzoic acid. |
| keywords:gallic acid antifungals synergy synthesis |
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