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Updated: May 23, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
New triazole derivatives as antifungal agents: synthesis via click reaction, in vitro evaluation and molecular
Yan Zou1, Qingjie Zhao, Jun Liao
1Department of Organic Chemistry, College of Pharmacy, Second Military Medical University, Shanghai, People's Republic of China.
Abstract:
A series of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols (5a-5y) which are analogues of fluconazole, have been designed and synthesized via Cu(I)-catalyzed azide-alkyne cycloaddition on the basis of computational docking experiments to the active site of the cytochrome P450 14α-demethylase (CYP51). The in vitro antifungal activities of all the target compounds were evaluated against eight human pathogenic fungi. Compound 5l showed the best antifungal activities.
