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Shichong Yu,Nan Wang,Xiaoyun Chai,Baogang Wang,Hong Cui,Qing-Jie Zhao,Yan Zou,Qingyan Sun,Qingguo Meng,Qiuye Wu 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.10
A series of fluconazole analogues containing1,2,3-triazole fragment have been designed and synthesizedon the basis of the active site of the cytochrome P45014a-demethylase (CYP51). Their structures were characterizedby 1H NMR, 13C NMR and LC–MS. The MIC80values indicate that the target compounds 1a–r showedhigher activities against nearly all the fungi tested to someextent except against Aspergillus fumigatus. Compounds1c, e, f, l and p showed 128 times higher activity (with theMIC80 value of 0.0039 mg/mL) than that of fluconazoleagainst Candida albicans and also showed higher activitythan that of the other positive controls.
Synthesis and Antifungal Activity of Novel Triazole Derivatives
Yongzheng Yan,Shichong Yu,Xiaoyun Chai,Honggang Hu,Qiuye Wu 대한약학회 2011 Archives of Pharmacal Research Vol.34 No.10
A series of novel azoles (a-v), which are analogues of fluconazole, have been designed and synthesized as potential antifungal agents by the click reaction. The click reaction approach toward the synthesis of novel 1,2,3-triazolyl linked triazole antifungal derivatives a-v was achieved by Cu(I)-catalyzed 1,3-dipolar cycloaddition of propargylated intermediate 5 with substituted azidomethyl benzene. In addition, the target compounds tested can increase antifungal activity.
Xiaoyun Chai,Qingyan Sun,Shichong Yu,Yongwei Jiang,Yan Zou,Qiuye Wu,Dazhi Zhang,Yuan-Ying Jiang,Yongbing Cao 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.11
A series of novel 1, 2, 4-triazole derivatives (9a-p) have been designed and synthesized as the potential antifungal agents. All compounds were characterized by 1H-NMR, 13C-NMR, and LCMS. Their antifungal activities against seven human pathogenic fungi were evaluated in vitro by measuring the minimal inhibitory concentrations. Most of the tested compounds were found to be more potent against Candida albicans than the control drug fluconazole.
Yan Zou,Qiuye Wu,Qingjie Zhao,Honggang Hu,Lina Hu,Shichong Yu,Mingjuan Xu 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.12
To explore the more active antitumor compounds, two series of new xanthones, containing 1,4-disubstituted-1,2,3-triazole moiety were designed and synthesized. Eaton’s Reagent and “click reaction” were used in the synthesis. Most of the title compounds showed good inhibitory activity against the hepatoma carcinoma cell line (Bel-7402) and human cervical carcinoma cell line (HeLa) in vitro. Compounds 10a, 10e, 10f, 11r and 11t had potent activity with IC50 values, ranging from 2.2 ± 0.17 to 7.1 ± 0.27 μM, which was equivalent to Doxorubicin.
Jun Liao,Fan Yang,Lei Zhang,Xiaoyun Chai,Qing-Jie Zhao,Shichong Yu,Yan Zou,Qingguo Meng,Qiuye Wu 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.4
A novel series of fluconazole based mimicsincorporating 1,3,4-oxadiazole moiety were designed andsynthesized. All the title compounds were characterized by1H-NMR, 13C-NMR, and Q-TOF-MS. Preliminary resultsrevealed that most of analogues exhibited significant antifungalactivity against seven pathogenic fungi. Compounds9g and 9k (MIC80 B 0.125 lg/mL, respectively) werefound more potent than the positive controls itraconazoleand fluconazole as broad-spectrum antifungal agents. Theobserved docking results showed that the 1,3,4-oxadiazolemoiety enhanced the affinity binding to the cytochromeP450 14a-demethylase (CYP51).