Synthesis and bioactivity evaluation of novel azoles containing dithiocarbamate moieties

被引：2
|
作者：
Fu, Ben [1 ]
Wu, Maocheng [1 ]
Huang, Lu [2 ]
Wu, Qiuye [1 ]
Wang, Shudong [2 ]
Chai, Xiaoyun [1 ]
机构：
[1] Second Mil Med Univ, Sch Pharm, Dept Organ Chem, Shanghai 200433, Peoples R China
[2] Nanjing Mil Command, Nanjing Gen Hosp, Dept Pharmaceut, Nanjing 210002, Jiangsu, Peoples R China
来源：
MEDICINAL CHEMISTRY RESEARCH | 2017年 / 26卷 / 10期
基金：
中国国家自然科学基金;
关键词：
Azole; Synthesis; Antifungal activity; CACYP51; ANTIFUNGAL AGENTS; BIOLOGICAL-ACTIVITIES; ISOTHIOCYANATES; DERIVATIVES; CANCER; CHEMISTRY; MECHANISM; DESIGN;
D O I：
10.1007/s00044-017-1948-0
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of novel azoles, N-methyl-N-[2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)]-propyl-(1-substituted phenyl)-dithiocarbamate has been designed, synthesized, and screened for antifungal activity by minimum inhibitory concentration. Results of preliminary antifungal tests showed that most of the title compounds had good antifungal activities against nearly all the tested fungal pathogens, especially against the Candida species. The most surprising finding of this study is that compound 4a, 4e, and 4k exhibited higher activities than fluconazole against Aspergillus fumigatus.
引用
收藏
页码：2491 / 2498
页数：8
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