Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability

Y Liu, Z Liu, X Cao, X Liu, H He, Y Yang

文献索引：Liu, Yu; Liu, Zining; Cao, Xufeng; Liu, Xin; He, Huili; Yang, Yushe Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 16 p. 4779 - 4783

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被引用次数: 10

摘要

To improve antifungal activities, water solubility and bioavailability, a series of novel analogues of itraconazole-containing pyridine rings were designed and synthesized. Their antifungal activities were evaluated in vitro against six clinically important fungi by measuring the minimal inhibitory concentrations (MICs). Most of the compounds showed more potent antifungal activities than that of itraconazole. In particular, the analogues 30d, ...