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KMID : 0043320110340101649
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Archives of Pharmacal Research
2011 Volume.34 No. 10 p.1649 ~ p.1656
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Synthesis and antifungal activity of novel triazole derivatives
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Yan Yongzheng
Yu Shichong
Chai Xiaoyun
Hu Honggang
Wu Qiuye
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Abstract
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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.
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KEYWORD
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Azole, Click reaction, Antifungal activity, CYP51
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