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  • Title: Synthesis and antifungal activity of the novel triazole derivatives containing 1,2,3-triazole fragment.
    Author: Yu S, Wang N, Chai X, Wang B, Cui H, Zhao Q, Zou Y, Sun Q, Meng Q, Wu Q.
    Journal: Arch Pharm Res; 2013 Oct; 36(10):1215-22. PubMed ID: 23640383.
    Abstract:
    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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