新型大环抗真菌剂的合成与生物活性：脂肽内酯FR901469鸟氨酸部分的酰化缀合物
Synthesis and biological activity of novel macrocyclic antifungals: acylated conjugates of the ornithine moiety of the lipopeptidolactone FR901469.
作者信息
Barrett D, Tanaka A, Harada K, Ohki H, Watabe E, Maki K, Ikeda F
机构信息
Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co. Ltd., Osaka, Japan.
出版信息
Bioorg Med Chem Lett. 2001 Feb 26;11(4):479-82. doi: 10.1016/s0960-894x(00)00705-8.
Abstract
A series of acylated analogues of the novel macrocyclic lipopeptidolactone FR901469 has been prepared and evaluated for antifungal and hemolytic activity. Several analogues displayed markedly reduced hemolytic potential and comparable protective effects to the natural product in a mouse model of candidiasis.
摘要
已制备了新型大环脂肽内酯FR901469的一系列酰化类似物，并对其抗真菌和溶血活性进行了评估。在念珠菌病小鼠模型中，几种类似物的溶血潜力显著降低，且与天然产物具有相当的保护作用。
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