|
KMID : 0043320130360101215
|
|
Archives of Pharmacal Research
2013 Volume.36 No. 10 p.1215 ~ p.1222
|
|
|
Synthesis and antifungal activity of the novel triazole derivatives containing 1,2,3-triazole fragment
|
|
Yu Shichong
Wang Nan
Chai Xiaoyun
Wang Baogang
Cui Hong
Zhao Qingjie
Zou Yan
Sun Qingyan
Meng Qingguo
Wu Qiuye
|
|
|
Abstract
|
|
|
|
A series of fluconazole analogues containing 1,2,3-triazole fragment have been designed and synthesized on the basis of the active site of the cytochrome P450 14α-demethylase (CYP51). Their structures were characterized by 1H NMR, 13C NMR and LC?MS. The MIC80 values indicate that the target compounds 1a?r showed higher activities against nearly all the fungi tested to some extent except against Aspergillus fumigatus. Compounds 1c, e, f, l and p showed 128 times higher activity (with the MIC80 value of 0.0039 mg/mL) than that of fluconazole against Candida albicans and also showed higher activity than that of the other positive controls.
|
|
|
KEYWORD
|
|
|
Synthesis, Triazole, Antifungal activity, CYP51
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
  
|