validamycin-a and Mycoses

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.

Topics: Animals; Antifungal Agents; Biological Products; Carbolines; Drug Discovery; Female; Humans; Male; Mice; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Mycoses; Protein Binding; Signal Transduction; Structure-Activity Relationship