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A series of novel 1,2,4-triazole derivatives with a 4-(4-substitutedphenyl) piperazine side chain were designed and synthesized based on the structure of lanosterol 14α-demethylase (CYP51). Their antifungal activities against eight human pathogenic fungi were evaluated in vitro by measuring the minimal inhibitory concentrations. Nearly all tested compounds were found to be more potent against Candida albicans than control drug fluconazole. Noticeably, the MIC(80) value of compounds 6,7,9,14 and 29 is 16 times lower than that of voriconazole against C. albicans. The activities of compounds 7 and 21 against Cryptococcus neoformans in vitro are comparable to that of voriconazole with a MIC(80) value of 0.0156 μg/mL. Moreover, the molecular model for the binding between compound 7 and the active site of CACYP51 was provided based on the computational docking results. Copyright © 2011 Elsevier Masson SAS. All rights reserved.


Jianming Xu, Yongbing Cao, Jun Zhang, Shichong Yu, Yan Zou, Xiaoyun Chai, Qiuye Wu, Dazhi Zhang, Yuanying Jiang, Qingyan Sun. Design, synthesis and antifungal activities of novel 1,2,4-triazole derivatives. European journal of medicinal chemistry. 2011 Jul;46(7):3142-8

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PMID: 21420761

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