唑类杂合抗真菌药物的研究进展  

Recent Developments in the Study of Novel Azole-Based Hybrid Antifungal Agents

作　　者：贺俊衡 周伟 He Jun-heng;Zhou Wei(College of Chemistry,Sichuan University,Chengdu 610065;College of Pharmaceutical Sciences,Southwest University,Chongqing 400715)

机构地区：[1]四川大学化学学院,成都610065 [2]西南大学药学院,重庆400715

出　　处：《国外医药(抗生素分册)》2024年第6期382-392,共11页World Notes on Antibiotics

基　　金：国家自然科学基金项目(项目编号:21702171)。

摘　　要：真菌感染,尤其是侵袭性真菌感染(IFI)已成为人类健康和世界卫生的重要威胁,每年有超过375万人死于IFI,这使得抗真菌药物的研制备受关注。唑类抗真菌药物是临床上使用范围最广的抗真菌药物,在治疗真菌感染中发挥着重要的作用,但传统唑类药物的毒副作用及长期用药产生的耐药性限制了唑类药物的进一步应用。开发新型杂合药物是抗真菌药物的一种极具潜力的策略,通过结合不同药物结构中的优势骨架,有望设计出具有优异抗耐药菌活性的新型抗真菌药物。本文对基于唑类结构设计的新型杂合抗真菌药物进行了综述,这些杂合药物在抗菌活性、抗耐药菌活性及低毒副作用等方面都展现出了可观的潜力,为新型抗真菌药物的研制提供了参考。Fungal infections,particularly invasive fungal infections(IFI),pose a significant threat to global health,resulting in over 1.5 million deaths annually.This alarming statistic underscores the urgent need to develop new antifungal drugs.In clinical practice,azole antifungals are the most often used class of antifungal medicines and are essential for treating fungal infections.However,the effectiveness of traditional azole drugs is often limited by toxic side effects and the emergence of long-term drug resistance.Hybrid drugs have emerged as a highly promising strategy for developing new antifungal agents.By integrating advantageous structural elements from different drugs,it is possible to design novel antifungal compounds with enhanced activity.This review focuses on recent advances in hybrid antifungal drugs based on azole structures.These hybrids have shown great promise in terms of reduced toxicity,action against drug-resistant fungus,and antifungal efficacy,providing important information for creating next-generation antifungal treatments.

关 键 词：抗真菌 杂合药物 唑类药物 双靶点 耐药性 CYP51 

分 类 号：R978.5[医药卫生—药品]