Liu Na, Wang Chen, Su Hua, Zhang Wannian, Sheng Chunquan
Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China.
Changhai Hospital of Traditional Chinese Medicine, Second Military Medical University, 800 Xiangyin Road, Shanghai 200433, China.
Future Med Chem. 2016 Aug;8(12):1435-54. doi: 10.4155/fmc-2016-0020. Epub 2016 Jul 27.
The development of next-generation antifungal agents with novel chemical scaffolds and new mechanisms of action is vital due to increased incidence and mortality of invasive fungal infections and severe drug resistance. This review will summarize current strategies to discover novel antifungal scaffolds. In particular, high-throughput screening, drug repurposing, antifungal natural products and new antifungal targets are focused on. New scaffolds with validated antifungal activity, their discovery and optimization process as well as structure-activity relationships are discussed in detail. Perspectives that could inspire future antifungal drug discovery are provided.
由于侵袭性真菌感染的发病率和死亡率上升以及严重的耐药性，开发具有新型化学骨架和新作用机制的下一代抗真菌药物至关重要。本综述将总结发现新型抗真菌骨架的当前策略。特别关注高通量筛选、药物再利用、抗真菌天然产物和新的抗真菌靶点。详细讨论了具有验证抗真菌活性的新骨架、它们的发现和优化过程以及构效关系。提供了可能启发未来抗真菌药物发现的观点。
