Synthesis and antifungal activity of N-aryl-substituted pimaricin derivatives

被引:0
作者
V. V. Belakhov
Yu. D. Shenin
B. I. Ionin
机构
[1] Technion – Israel Institute of Technology,Schulich Faculty of Chemistry
[2] All-Russia Research Institute of Plant Protection,undefined
[3] St. Petersburg Technological Institute,undefined
来源
Pharmaceutical Chemistry Journal | 2010年 / 44卷
关键词
polyene macrolide antibiotics; pimaricin; -acyl-substituted derivatives; antifungal activity;
D O I
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中图分类号
学科分类号
摘要
Reactions of the tetraene macrolide antibiotic pimaricin with 1-fluorobenzenes resulted in the formation of N-aryl-substituted derivatives. The physicochemical and biological properties of the synthesized pimaricin derivatives were studied. The N-aryl-substituted pimaricin derivatives showed high antifungal activity against a broad spectrum of test cultures. The biological studies showed that the acute toxicity (LD50) of the obtained pimaricin derivatives was half that of the starting antibiotic.
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页码:486 / 492
页数:6
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