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Synthesis and antifungal activity of the novel triazole derivatives containing 1,2,3-triazole fragment. 2013
Shichong Yu, and
Nan Wang, and
Xiaoyun Chai, and
Baogang Wang, and
Hong Cui, and
Qingjie Zhao, and
Yan Zou, and
Qingyan Sun, and
Qingguo Meng, and
Qiuye Wu
Department of Organic Chemistry, College of Pharmacy, Second Military Medical University, Guohe Road 325, Shanghai, 200433, People's Republic of China.
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.
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