Synthesis and antifungal activities of novel triazole derivatives
-
摘要: 目的 研究具有萘苄结构的三唑醇类化合物的抗真菌活性。 方法 设计合成了9个目标化合物;其结构通过1H NMR、MS确证,选择8种真菌为实验菌株,根据美国国家临床实验室标准委员会(NCCLS)推荐的标准化抗真菌敏感性实验方法,进行体外抑菌活性测试。 结果 所有化合物对所选真菌均表现出了一定的抑菌活性,化合物1c对除烟曲霉菌以外的其他7种真菌的MIC80值<0.125 μg/ml,是伏立康唑活性的16倍。 结论 引入萘环和烃基侧链的目标化合物都有抗真菌活性。Abstract: Objective To synthesize a new series of triazole compounds with naphthalene benzyl as side chain and evaluate the antifungal activity. Methods Nine title compounds were synthesized and determined by the 1H NMR and MS spectra. According to the method recommended by the national committee for clinical laboratory standards(NCCLS), the RPMI-1640 test medium was used,the antifungal activities of all the compounds were evaluated against eight human pathogenic fungi in vitro. Results The title compounds exhibited potent antifungal activities. Compound 1c showed high activities against 7 funguses except Aspergillus fumigatus with the MIC80 values less than 0.125 μg/ml, which was 16 times higher than that of Voriconazole. Conclusion The title compounds with naphthalene and alkyl substituent showed potent antifungal activities.
-
Key words:
- triazole derivatives /
- chemical synthesis /
- antifungal activity
-
[1] Zou Y, Yu S, Li R, et al. Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates[J].Eur J Med Chem, 2014,74(3):366-374. [2] Tang H, Zheng CH, Ren XH, et al. Synthesis and biological evaluation of novel triazole derivatives as antifungal agents[J].Chin Chem Lett, 2013,24(3): 219-222. [3] Wang S, Jin G, Wang W, et al.synthesis and structure-activity relationships of new triazole derivatives containing N-substituted phenoxypropylamino side chains[J]. Eur J Med Chem, 2012,53(4): 292-299. [4] Zou Y, Zhao Q, Liao J, et al. New triazole derivatives as antifungal agents: synthesis via click reaction, in vitro evaluation and molecular docking studies[J].Bioorg Med Chem Lett, 2012,22(8):2959-2962. [5] Jiang Y, Zhang J, Cao Y,et al. Synthesis, in vitro evaluation and molecular docking studies of new triazole derivatives as antifungal agents[J]. Bioorg Med Chem Lett,2011, 21(15): 4471-4475. [6] Chai X, Zhang J, Cao Y,et al. Design, synthesis and molecular docking studies of novel triazole as antifungal agent[J]. Eur J Med Chem, 2011, 46(7): 3167-3176. [7] National Committee for Clinical Laboratory Standards.Reference method for broth dilution antifungal susceptibility testing of yeasts approved standard[S]. Document M27-A2, Wayne, PA, 2002. -
点击查看大图
计量
- 文章访问数: 2005
- HTML全文浏览量: 232
- PDF下载量: 74
- 被引次数: 0
下载:
