Natural and synthetic β-carboline as a privileged antifungal scaffolds

Eur J Med Chem. 2022 Feb 5:229:114057. doi: 10.1016/j.ejmech.2021.114057. Epub 2021 Dec 17.

Abstract

The discovery of antifungal agents with novel structure, broad-spectrum, low toxicity, and high efficiency has been the focus of medicinal chemists. Over the past decades, β-carboline scaffold has attracted extensive attention in the scientific community due to its potent and diverse biological activities with nine successfully marketed β-carboline-based drugs. In this review, we summarized the current states and advances in the antifungal activity of natural and synthetic β-carbolines. Additionally, the structure-activity relationships and their antifungal mechanisms targeting biofilm, cell wall, cell membrane, and fungal intracellular targets were also systematically discussed. In summary, β-carbolines have the great potential to develop new efficient scaffolds to combat fungal infections.

Keywords: Antifungal; Mechanism; Structure-activity relationships; β-carboline.

Publication types

  • Review

MeSH terms

  • Animals
  • Antifungal Agents / chemistry*
  • Antifungal Agents / pharmacology
  • Biological Products / chemistry*
  • Biological Products / pharmacology
  • Carbolines / chemical synthesis*
  • Carbolines / pharmacology
  • Drug Discovery
  • Female
  • Humans
  • Male
  • Mice
  • Microbial Sensitivity Tests
  • Models, Molecular
  • Molecular Structure
  • Mycoses / drug therapy*
  • Protein Binding
  • Signal Transduction
  • Structure-Activity Relationship

Substances

  • Antifungal Agents
  • Biological Products
  • Carbolines