Synthesis and antifungal activity of the novel triazole compounds
Synthesis and antifungal activity of the novel triazole compounds
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DOI：
10.1039/c3md20086h
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发表时间：
2013-04-01
期刊：
影响因子：
--
通讯作者：
Wu, Qiuye
中科院分区：
文献类型：
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作者：
Yu, Shichong;Chai, Xiaoyun;Wu, Qiuye
基于细胞色素P450 14 α-去甲基酶（CYP51）活性位点的计算对接实验，首次通过点击反应设计并合成了一系列氟康唑类似物1-(1H-1,2,4-三唑-1-基)-2-(2,4-二氟苯基)-3-取代-2-丙醇(1a-o)。通过H-1 NMR、C-13 NMR和HRMS对其结构进行了表征。评估了所有目标化合物针对八种人类病原真菌的体外抗真菌活性。
A series of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols (1a-o) which are analogues of fluconazole, have been designed and synthesized for the first time by the click reaction on the basis of computational docking experiments to the active site of the cytochrome P450 14 alpha-demethylase (CYP51). Their structures were characterized by H-1 NMR, C-13 NMR and HRMS. The in vitro antifungal activities of all the target compounds were evaluated against eight human pathogenic fungi.