Design, synthesis, and biological evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14α-demethylase

X Chai, J Zhang, H Hu, S Yu, Q Sun, Z Dan…

文献索引：Chai, Xiaoyun; Zhang, Jun; Hu, Honggang; Yu, Shichong; Sun, Qingyan; Dan, Zhigang; Jiang, Yuanying; Wu, Qiuye European Journal of Medicinal Chemistry, 2009 , vol. 44, # 5 p. 1913 - 1920

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被引用次数: 35

摘要

Based on the results of computational docking to the active site of the cytochrome P450 14α- demethylase (CYP51), a series of 1-(1H-1, 2, 4-triazole-1-yl)-2-(2, 4-difluorophenyl)-3- substituted-2-propanols as analogs of fluconazole were designed, synthesized, and evaluated as antifungal agents. The MIC80 values indicate that compounds 1a–n exhibited higher activity against nearly all fungi tested except Aspergillus fumigatus than ...