Synthesis and antifungal activity of the novel triazole derivatives containing 1,2,3-triazole fragment

• DOI: 10.1007/s12272-013-0063-0
• Publication Date: 2013-05-02T16:40:40Z
• Authors: Shichong Yu; Nan Wang; Xiaoyun Chai; Baogang Wang; Hong Cui; Qingjie Zhao; Yan Zou; Qingyan Sun; Qingguo Meng; Qiuye Wu
• Keywords: Triazole; 1,2,4-Triazole

A series of fluconazole analogues containing 1,2,3-triazole fragment have been designed and synthesized on the basis of the active site of the cytochrome P450 14α-demethylase (CYP51). Their structures were characterized by (1)H NMR, (13)C NMR and LC-MS. The MIC80 values indicate that the target compounds 1a-r showed higher activities against nearly all the fungi tested to some extent except against Aspergillus fumigatus. Compounds 1c, e, f, l and p showed 128 times higher activity (with the MIC80 value of 0.0039 mg/mL) than that of fluconazole against Candida albicans and also showed higher activity than that of the other positive controls.