New coumarin derivatives accessible in short and eco-friendly conditions with antifungal activity

Future Med Chem. 2023 May;15(9):745-756. doi: 10.4155/fmc-2023-0033. Epub 2023 May 25.

Abstract

Aim: The synthesis of a novel class of compounds bearing a coumarin entity was targeted. They are either iminocoumarins or characterized by the presence of a pyridone ring fused within the iminocoumarin scaffold. Methods & results: The targeted compounds were synthesized through a short method, thanks to microwave activation. The study evaluated the antifungal activity of 13 newly synthesized compounds against a new fungal strain of Aspergillus niger. The most active compound showed activity comparable to the widely used reference drug, amphotericin B. Conclusion: The conditions and the ease of synthesis warrant high potential of the method for diversity-oriented synthesis, very useful within the drug discovery area.

Keywords: Aspergillus niger; antifungal activity; coumarins; iminocoumarins.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antifungal Agents* / pharmacology
  • Coumarins / pharmacology
  • Fungi*
  • Microbial Sensitivity Tests
  • Microwaves
  • Structure-Activity Relationship

Substances

  • Antifungal Agents
  • Coumarins