Synthesis and antifungal activity of novel triazole derivatives

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)-ca...

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Bibliographic Details
Published in:Archives of pharmacal research 2011, 34(10), , pp.1649-1656
Main Authors: Yan, Yongzheng, Yu, Shichong, Chai, Xiaoyun, Hu, Honggang, Wu, Qiuye
Format: Article
Language:English
Subjects:
14-alpha Demethylase Inhibitors - chemical synthesis
14-alpha Demethylase Inhibitors - pharmacology
Antifungal Agents - chemical synthesis
Antifungal Agents - pharmacology
Catalysis
Copper
Fungi - drug effects
Fungi - enzymology
Indicators and Reagents
Magnetic Resonance Spectroscopy
Medicine
Microbial Sensitivity Tests
Pharmacology/Toxicology
Pharmacy
Spectrophotometry, Infrared
Structure-Activity Relationship
Triazoles - chemical synthesis
Triazoles - pharmacology
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Summary: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.
ISSN:0253-6269
1976-3786
DOI:10.1007/s12272-011-1009-z