抗真菌药物氟康唑研究新进展  

Recent advances in antifungal fluconazole

作　　者：万昆[1] 张奕奕[1] 周成合[1] 周向东[2] 耿蓉霞[1] 吉庆刚[1] 

机构地区：[1]西南大学化学化工学院,重庆400715 [2]第三军医大学药学院,重庆400038

出　　处：《中国抗生素杂志》2012年第1期8-15,20,共9页Chinese Journal of Antibiotics

基　　金：国家自然科学基金(21172181);中央高校基本科研业务费专项资金(XDJK2009C092);高等学校博士学科点专项科研基金(SRFDP20110182110007);人事部回国人员重点项目(2002-99);西南大学基金(SWUB2006018;XSGX0602)资助

摘　　要：氟康唑作为一种广谱的三唑类抗真菌药物,因其毒副作用小、对深部真菌感染疗效显著及药代动力学好等特点,成为WHO指定的治疗全身性真菌感染的首选药物。随着氟康唑的广泛使用,对其进行深入研究与开发也日趋活跃,已取得了众多杰出成果,显示出了其在医药领域的巨大开发价值和潜在的宽广应用。本文结合自己的工作,参考国内外文献总结了近些年来抗真菌药物氟康唑的研究与开发新近况,主要包括:(1)合成方法研究;(2)结构优化和修饰研究;(3)超分子化学及其超分子药物开发研究;(4)临床用药研究;并对其发展趋势与前景做了展望,希望有助于氮唑类抗真菌药物的进一步发展。Fluconazole, as a broad-spectrum antifungal drug, has become a first choice to treat systemic fungal infection in WHO recommendation due to its low toxicity, excellent safety profile and favorable pharmacokinetic characteristics. Along with the wide use of Fluconazole, many achievements have been acquired and the researches are becoming increasingly active. Combining with our researches and referring to other published literatures in recent years, this review summarized the recent progress of researches and developments in the antifungal Fluconazole, mainly including （1） the synthetic methods; （2） the structure optimization and modification; （3） the developments of supramolecular chemistry and supramolecular drugs; （4） the researches of clinical medication. The perspectives of the foreseeable future of Fluconazole are also presented, hoping it can serve as a stimulant for the further development of nitrogen azoles.

关 键 词：氟康唑 合成 超分子 抗真菌 抗癌 

分 类 号：R978.5[医药卫生—药品]