Design, synthesis, and antifungal activities of novel triazole derivatives containing the benzyl group

Drug Des Devel Ther. 2015 Mar 11:9:1459-67. doi: 10.2147/DDDT.S74989. eCollection 2015.

Abstract

In previous studies undertaken by our group, a series of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols (1a-r), which were analogs of fluconazole, was designed and synthesized by click chemistry. In the study reported here, the in vitro antifungal activities of all the target compounds were evaluated against eight human pathogenic fungi. Compounds 1a, 1q, and 1r showed the more antifungal activity than the others.

Keywords: CYP51; antifungal activity; synthesis; triazole.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antifungal Agents / chemical synthesis*
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology*
  • Aspergillus fumigatus / drug effects
  • Benzyl Compounds / chemistry*
  • Candida albicans / drug effects
  • Candida glabrata / drug effects
  • Dose-Response Relationship, Drug
  • Drug Design*
  • Microbial Sensitivity Tests
  • Microsporum / drug effects
  • Molecular Structure
  • Structure-Activity Relationship
  • Triazoles / chemical synthesis*
  • Triazoles / chemistry
  • Triazoles / pharmacology*

Substances

  • Antifungal Agents
  • Benzyl Compounds
  • Triazoles