抗真菌药物氟康唑研究新进展.pdf

. 8 . 中国抗生素杂志2012年1月第37卷第1期 文章编号：1001-8689(2012)01-0008-08 抗真菌药物氟康唑研究新进展 1 1 1,* 2 1 1 万昆 张奕奕 周成合 周向东 耿蓉霞 吉庆刚 (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) 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。 关键词：氟康唑；合成；超分子；抗真菌；抗癌 中图分类号：R978.5 文献标识码：A Recent advances in antifungal fl uconazole 1 1 1 2 1 1 Wan Kun , Zhang Yi-yi , Zhou Cheng-he , Zhou Xiang-dong , Geng Rong-xia and Ji Qing-gang (1 School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715; 2 School of Pharmaceutical Sciences, Third Military Medical University, Chongqing 400038) Abstract Fluconazole, as a broad-spectrum antifungal drug, has become a fi rst 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 modifi cation; (3) the developments