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目的:研究具有环丙基结构的三唑醇类化合物的抗真菌活性。方法:设计合成了9个三唑醇类新化合物,所有目标化合物结构都通过1H NMR、MS和元素分析验证;选择8种真菌为实验菌株,进行体外抑菌活性测试。结果:目标化合物对8种真菌特别是深部真菌均有比较强的抑制活性,所有目标化合物对白念珠菌的MIC80值<0.125μg/ml,是氟康唑活性的4倍以上,与伊曲康唑活性相当。结论:1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluoro-phenyl)-3-[N-cyclopropyl-N-(3,4-dichlorobenzyl)amino]-propanol(化合物6f)的活性比较好,有进一步研究开发的价值。
Objective: To study the antifungal activity of triadimenol with cyclopropyl structure. Methods: Nine new triazole compounds were designed and synthesized. The structures of all target compounds were confirmed by 1H NMR, MS and elemental analysis. Eight kinds of fungi were selected as experimental strains to test the antibacterial activity in vitro. Results: The target compounds exhibited strong inhibitory activity against eight fungi, especially deep fungi. The MIC80 values of all the target compounds against Candida albicans were <0.125μg / ml, more than four times higher than that of fluconazole, Activity is quite. CONCLUSION: 1- (1H-1,2,4-triazole-1-yl) -2- [2,4- difluoro-phenyl] -3- [N-cyclopropyl- The activity of -propanol (compound 6f) is relatively good, with further research and development value.