| 1-(1 H-1, 2, 4-三唑-1-基)-2-(2, 4-二氟苯基)-3-[N-异丙基-N-(4-取代苄基)]-2-丙醇的合成及抗真菌活性 |
| 投稿时间：2010-12-28 修订日期：2011-05-30 点此下载全文 |
| 引用本文：闫永正,柴晓云,邹燕,俞世冲,吴秋业.1-(1 H-1, 2, 4-三唑-1-基)-2-(2, 4-二氟苯基)-3-[N-异丙基-N-(4-取代苄基)]-2-丙醇的合成及抗真菌活性[J].药学实践杂志,2011,29(5):358~361 |
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| 基金项目:国家自然科学基金资助项目(20972188), 上海市科委中药现代化基金专项(09dZ1976700), 上海市重点学科资助项目(B906). |
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| 中文摘要:目的 研究具有异丙基结构的氮唑类化合物的抗真菌活性。 方法 引入4位羧酸酯取代的苄基侧链结构, 合成一系列目标化合物,所有化合物结构均经MS、1H-NMR等谱确证;选择8种真菌为实验菌株,测定其体外抗真菌活性。 结果 合成了14个未见文献报道的目标化合物;所有化合物对所选真菌均表现出了一定的抑菌活性,其中化合物(1)和(2)对除薰烟曲霉菌外的7种菌都表现出了较好的抑菌活性。 结论 4位羧酸酯取代的苄基侧链结构的引入对目标化合物的抗菌活性有一定的影响,侧链越短,抑菌活性越好。 |
| 中文关键词:氮唑类 化学合成 抗真菌活性 |
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| 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluoroph-enyl)-3-(N-cycloproyl-N-benzyl-amino)-2-propanols |
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| Abstract:Objective To study the antifungal activity of triazole alcohols which introduce isopropyl as side chain. Methods By introduction of 4-carboxylic ester substituted benzyl group as side chain, a series of title compounds were synthesized. All of them were confirmed by MS, 1H-NMR, et al. The antifungal activities were also evaluated against eight tested pathogenic fungi. Results Fourteen title compounds were synthesized. All title compounds exhibited activity against tested fungi to some extent. Compounds (1) and (2) exhibited stronger antifungal activities against eight fungi except Aspergillus fumigatus than the control drug of itraconazole. Conclusions The introduction of 4-carboxylic ester substituted benzyl group as side chain was beneficial to improve their antifungal activity. The shorter in the side chain , the better of the antifungal activity. |
| keywords:azoles chemical synthesis antifungal activity |
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