Synthesis and antifungal activity of novel triazole derivatives

Arch Pharm Res. 2011 Oct;34(10):1649-56. doi: 10.1007/s12272-011-1009-z. Epub 2011 Nov 12.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 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
  • Microbial Sensitivity Tests
  • Spectrophotometry, Infrared
  • Structure-Activity Relationship
  • Triazoles / chemical synthesis*
  • Triazoles / pharmacology*

Substances

  • 14-alpha Demethylase Inhibitors
  • Antifungal Agents
  • Indicators and Reagents
  • Triazoles
  • Copper