Design, synthesis and antifungal evaluation of 1-(2-(2, 4-difluorophenyl)-2-hydroxy-3-(1H-1, 2, 4-triazol-1-yl) propyl)-1H-1, 2, 4-triazol-5 (4H)-one

Y Jiang, Y Cao, J Zhang, Y Zou, X Chai, H Hu…

文献索引：Jiang, Yongwei; Cao, Yongbin; Zhang, Jun; Zou, Yan; Chai, Xiaoyun; Hu, Honggang; Zhao, Qingjie; Wu, Qiuye; Zhang, Dazhi; Jiang, Yuanying; Sun, Qingyan European Journal of Medicinal Chemistry, 2011 , vol. 46, # 7 p. 3135 - 3141

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被引用次数: 17

摘要

Based on the structure of the active site of cytochrome P450 14α-demethylase (CYP51) and the conclusions of the structure-activity relationships of azole antifungals, a series of 1-(2-(2, 4-difluoro-phenyl)-2-hydroxy-3-(1H-1, 2, 4-triazol-1-yl) propyl)-1H-1, 2, 4-triazol-5 (4H)-one of fluconazole analogs was synthesized. All compounds were characterized by IR, HRMS, 1HNMR and 13C NMR spectroscopic analysis. Results of preliminary antifungal in vitro ...