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.

发现结构新颖、广谱、低毒、高效的抗真菌药物一直是药物化学家关注的焦点。在过去的几十年里，β-咔啉支架因其强大而多样的生物活性而引起了科学界的广泛关注，其中有九种成功上市的β-咔啉类药物。在这篇综述中，我们总结了天然和合成β-咔啉的抗真菌活性的现状和进展。此外，还系统地讨论了针对生物膜、细胞壁、细胞膜和真菌细胞内靶点的构效关系及其抗真菌机制。总之，β-咔啉具有开发新的有效支架以对抗真菌感染的巨大潜力。