State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Taipa, Macau SAR, China; College of Veterinary Medicine, Northwest A&F University, Shaanxi, China; School of Life Science and Technology, Weifang Medical University, Shandong, China.
School of Life Science and Technology, Weifang Medical University, Shandong, China.
Eur J Med Chem. 2022 Feb 5;229:114057. doi: 10.1016/j.ejmech.2021.114057. Epub 2021 Dec 17.
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.
新型结构、广谱、低毒、高效的抗真菌药物的发现一直是药物化学家关注的焦点。在过去的几十年中，β-咔啉支架由于其具有强大而多样的生物活性，已经有 9 种基于β-咔啉的药物成功上市，因此引起了科学界的广泛关注。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结构-活性关系及其抗真菌机制。总之，β-咔啉具有开发新型高效抗真菌药物的巨大潜力。
