期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 46, 期 7, 页码 3142-3148出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.02.042
关键词
Synthesis; Antifungal activity; 1,2,4-Triazole; Piperazine
资金
- National Natural Science Foundation of China [30300437, 20772153]
- Eleventh Five Year Military Medicine and Public Health Research Projects [06MB206]
- Shanghai Leading Academic Discipline Project [B906]
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 14 alpha-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 MIC80 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 MIC80 value of 0.0156 mu g/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. (C) 2011 Elsevier Masson SAS. All rights reserved.
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