新型三唑类化合物的设计、合成和抗真菌活性研究

李洋洋; 刘华; 刘宏; 张永强; 张万年; 盛春泉

doi:10.3969/j.issn.1006-0111.2013.01.008

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新型三唑类化合物的设计、合成和抗真菌活性研究

李洋洋, 刘华, 刘宏, 张永强, 张万年, 盛春泉

文章导航 > 药学实践与服务 > 2013 > 31(1): 27-31

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]. 药学实践与服务, 2013, 31(1): 27-31. doi: 10.3969/j.issn.1006-0111.2013.01.008

引用本文:

LI Yang-yang, LIU Hua, LIU Hong, ZHANG Yong-qiang, ZHANG Wan-nian, SHENG Chun-quan. Design, synthesis and antifungal activity of novel triazole derivatives[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(1): 27-31. doi: 10.3969/j.issn.1006-0111.2013.01.008

Citation:

LI Yang-yang, LIU Hua, LIU Hong, ZHANG Yong-qiang, ZHANG Wan-nian, SHENG Chun-quan. Design, synthesis and antifungal activity of novel triazole derivatives[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(1): 27-31. doi: 10.3969/j.issn.1006-0111.2013.01.008

新型三唑类化合物的设计、合成和抗真菌活性研究

doi: 10.3969/j.issn.1006-0111.2013.01.008

1.
江西中医学院药物化学学科组, 江西南昌330006
2.
第二军医大学药学院药物化学教研室, 上海 200433

基金项目: 国家自然科学基金重点项目(30930107).

Design, synthesis and antifungal activity of novel triazole derivatives

1.
Department of Medicinal Chemistry, Jiangxi institute of traditional Chinese medicine, Nanchang 330006, China
2.
Department of Medicinal Chemistry, Second Military Medicinal University, Shanghai 200433, China

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。
- 三唑 /
- 三唑酮侧链 /
- 化学合成 /
- 抗真菌活性
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.
- triazole /
- triazolone side chain /
- chemical synthesis /
- antifungal activities

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[2]	Borate HB, Maujan SR, Sawargave SP, et al. Fluconazole analogues containing 2H-1,4-benzothiazin-3(4H)-one or 2H-1,4-benzoxazin-3(4H)-one moieties, a novel class of anti-Candida agents[J]. Bioorg Med Chem Lett,2010, 20(2):722.
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新型三唑类化合物的设计、合成和抗真菌活性研究

doi: 10.3969/j.issn.1006-0111.2013.01.008

1. 江西中医学院药物化学学科组, 江西南昌330006

2. 第二军医大学药学院药物化学教研室, 上海 200433

基金项目: 国家自然科学基金重点项目(30930107).

收稿日期: 2012-06-01
修回日期: 2012-09-21

关键词:

三唑 /

三唑酮侧链 /

化学合成 /

抗真菌活性

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。