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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

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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: 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
shu
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
shu

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。
    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.
  • [1] Sheng C, Zhang W. New Lead Structures in Antifungal Drug Discovery[J]. Curr Med Chem,2011, 18(5): 733.
    [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.
    [3] Guillon R, Pagniez F, Rambaud C, et al. Design, synthesis, and biological evaluation of 1-[(biarylmethyl)methylamino]-2-(2,4-difluorophenyl)-3- (1H-1,2,4-triazol-1-yl)propan-2-ols as potent antifungal agents: new insights into structure-activity relationships[J]. Chem Med Chem,2011, 6(10):1806.
    [4] Guillon R, Pagniez F, Giraud F, et al. Design, synthesis, and in vitro antifungal activity of 1-[(4-substituted-benzyl)methylamino]-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ols[J].Chem Med Chem,2011, 6(5):816.
    [5] Sheng C, Zhang W, Zhang M, et al. Homology Modeling of Lanosterol 14-Demethylase of Candida albicans and Aspergillus fumigatus and Insights into the Enzyme-Substrate Interactions[J]. J Biomol Struct & Dyn, 2004, 22(1):91.
    [6] Sheng C, Wang W, Che X, et al. Improved Model of Lanosterol 14alpha-Demethylase by LigandSupported Homology Modeling: Validation by Virtual Screening and Azole Optimization[J]. Chem Med Chem,2010, 5(3): 390.
    [7] Sheng C, Miao Z, Ji H, Threedimensional model of lanosterol 14 alpha-demethylase from Cryptococcus neoformans: activesite characterization and insights into azole binding. Antimicrob Agents[J].Chemother,2009, 53(8):3487.
    [8] Sheng C, Zhang W, Ji H, et al. Structure-based Optimization of Azole Antifungal Agents by CoMFA, CoMSIA and Molecular Docking[J]. J Med Chem, 2006, 49(8):2512.
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  • 收稿日期:  2012-06-01
  • 修回日期:  2012-09-21

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

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。

English Abstract

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: 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
shu
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
shu

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