Functionalised isocoumarins as antifungal compounds: Synthesis and biological studies

Bioorg Med Chem Lett. 2016 Jan 1;26(1):235-9. doi: 10.1016/j.bmcl.2015.08.086. Epub 2015 Aug 31.


A series of novel 3-substituted isocoumarins was prepared via Pd-catalysed coupling processes and screened in vitro for antifungal activity against Candida species. The study revealed antifungal potential of isocoumarins possessing the azole substituents, which, in some cases, showed biological properties equal to those of clinically used voriconazole. Selected compounds were also screened against voriconazole resistant Candida krusei 6258 and a clinical isolate Candida parapsilosis CA-27. Although the activity against these targets needs to be improved further, the results emphasise additional potential of this new class of antifungal compounds.

Keywords: Antifungal compounds; Candida species; Isocoumarin derivatives.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antifungal Agents / chemical synthesis*
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology*
  • Candida / cytology
  • Candida / drug effects*
  • Cell Line
  • Cell Survival / drug effects
  • Dose-Response Relationship, Drug
  • Humans
  • Isocoumarins / chemical synthesis*
  • Isocoumarins / chemistry
  • Isocoumarins / pharmacology*
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Structure-Activity Relationship


  • Antifungal Agents
  • Isocoumarins