| 新型三唑类化合物的设计、合成和抗真菌活性研究 |
| 投稿时间：2012-06-01 修订日期：2012-09-21 点此下载全文 |
| 引用本文：李洋洋,刘华,刘宏,张永强,张万年,盛春泉.新型三唑类化合物的设计、合成和抗真菌活性研究[J].药学实践杂志,2013,31(1):27~31 |
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| 基金项目:国家自然科学基金重点项目(30930107). |
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| 中文摘要:目的 基于唑类药物合理优化的分子设计模型,设计新型三唑类化合物,并测试其对常见致病真菌的抑制活性。方法 采用环氧化物开环法合成目标化合物,通过1H NMR和MS确证其化学结构,经微量液基稀释法测试体外抗真菌活性。结果 合成了2个含三唑酮侧链的新型唑类化合物,它们均显示了优秀的广谱抗真菌活性。结论 目标化合物对白色念珠菌的活性优于对照药氟康唑和酮康唑,值得进一步深入构效关系研究。 |
| 中文关键词:三唑 三唑酮侧链 化学合成 抗真菌活性 |
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| Design, synthesis and antifungal activity of novel triazole derivatives |
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| Abstract:Objective To design the novel triazole derivatives and test their in vitro antifungal activities on the basis of the molecular design model for rational optimization of azole drugs.Methods Ring-open reaction of the oxiranes was used to synthesize the target compounds, whose chemical structures were confirmed by 1H NMR and MS. Serial dilution method was used to determine the in vitro antifungal activities. Results Two novel azole compounds containing trizaolone side chains were synthesized which showed excellent and broad-spectrum antifungal activity. Conclusion The targeted compounds showed better antifungal activity against Candida albicans than the positive drugs fluconazole and ketoconazole, which was worth to further investigate the structure-activity relationship. |
| keywords:triazole triazolone side chain chemical synthesis antifungal activities |
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