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Volume 31 Issue 3
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Article Navigation >  Journal of Pharmaceutical Practice and Service  > 2013  >  31(3): 176-180

XU Bo, SHI Yuan, ZHANG Wan-nian, SHENG Chun-quan. Design, synthesis and antifungal activity of novel triazole derivatives with piperazine side chain[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(3): 176-180. doi: 10.3969/j.issn.1006-0111.2013.03.004
Citation: XU Bo, SHI Yuan, ZHANG Wan-nian, SHENG Chun-quan. Design, synthesis and antifungal activity of novel triazole derivatives with piperazine side chain[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(3): 176-180. doi: 10.3969/j.issn.1006-0111.2013.03.004
shu

Design, synthesis and antifungal activity of novel triazole derivatives with piperazine side chain

doi: 10.3969/j.issn.1006-0111.2013.03.004
  • 1.

    Department of Medicinal Chemistry, Second Military Medicinal University, Shanghai 200433, China

  • 2.

    Third People's Hospital of Chongming, Shanghai 202150, China

  • Received Date: 2012-09-08
  • Rev Recd Date: 2012-11-14
  • Objective To design novel diazole derivatives on the basis of the binding mode of azole antifungal agents with the target enzyme and test their in vitro antifungal activities. Methods Acylation reaction of the oxidants 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 Twelve novel azole compounds containing C1 methyl group and piperazine side chains were synthesized, which showed moderate to good antifungal activity. Conclusion Several target compounds showed better antifungal activity against Candida albicans than the positive drug fluconazole, which were worth to further investigating 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] 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.
    [3] Sheng C, Wang W, Che X, et al. Improved model of lanosterol 14alpha-demethylase by ligand-supported homology modeling:validation by virtual screening and azole optimization. ChemMedChem[J]. 2010, 5(3):390.
    [4] Sheng C, Miao Z, Ji H, et al. Three-dimensional model of lanosterol 14 alpha-demethylase from Cryptococcus neoformans:active-site characterization and insights into azole binding[J]. Antimicrob Agents Chemother. 2009, 53(8):3487.
    [5] 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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Design, synthesis and antifungal activity of novel triazole derivatives with piperazine side chain

doi: 10.3969/j.issn.1006-0111.2013.03.004
  • 1. Department of Medicinal Chemistry, Second Military Medicinal University, Shanghai 200433, China
  • 2. Third People's Hospital of Chongming, Shanghai 202150, China
  • Received Date: 2012-09-08
  • Rev Recd Date: 2012-11-14

Abstract: Objective To design novel diazole derivatives on the basis of the binding mode of azole antifungal agents with the target enzyme and test their in vitro antifungal activities. Methods Acylation reaction of the oxidants 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 Twelve novel azole compounds containing C1 methyl group and piperazine side chains were synthesized, which showed moderate to good antifungal activity. Conclusion Several target compounds showed better antifungal activity against Candida albicans than the positive drug fluconazole, which were worth to further investigating the structure-activity relationship.

XU Bo, SHI Yuan, ZHANG Wan-nian, SHENG Chun-quan. Design, synthesis and antifungal activity of novel triazole derivatives with piperazine side chain[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(3): 176-180. doi: 10.3969/j.issn.1006-0111.2013.03.004
Citation: XU Bo, SHI Yuan, ZHANG Wan-nian, SHENG Chun-quan. Design, synthesis and antifungal activity of novel triazole derivatives with piperazine side chain[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(3): 176-180. doi: 10.3969/j.issn.1006-0111.2013.03.004
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