先导物导向合成及新型埃兰斯碱衍生物的生物评价。
Precursor-directed syntheses and biological evaluation of new elansolid derivatives.
机构信息
Helmholtz Centre for Infection Research, Research Group Microbial Drugs, Inhoffenstrasse 7, 38124 Braunschweig, Germany.
出版信息
Chembiochem. 2012 Aug 13;13(12):1813-7. doi: 10.1002/cbic.201200228. Epub 2012 Jul 17.
The antibiotic elansolid C1 (8) was isolated from Chitinophaga sancti strain FxGBF13 after fermentation in the presence of anthranilic acid. Remarkably, 8 was also obtained by addition of anthranilic acid to a crude fermentation extract containing the macrolide elansolid A2 (1*). This Michael-type conjugate addition allowed us to generate 21 new derivatives of elansolid C1 (9-29) by using various nucleophiles. Biological activities of all derivatives were evaluated against Staphylococcus aureus, Micrococcus luteus, and the mouse cell line L929.
抗生素 elansolid C1（8）是在存在邻氨基苯甲酸的情况下，从 Chitinophaga sancti 菌株 FxGBF13 发酵中分离得到的。值得注意的是，通过向含有大环内酯 elansolid A2（1*）的粗发酵提取物中添加邻氨基苯甲酸，也可以得到 8。这种迈克尔型共轭加成反应允许我们使用各种亲核试剂生成 21 种 elansolid C1（9-29）的新衍生物。所有衍生物的生物活性均针对金黄色葡萄球菌、藤黄微球菌和小鼠细胞系 L929 进行了评估。
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