红霉素2'-酯的抗菌活性
Antibacterial activity of 2'-esters of erythromycin.
作者信息
Tardrew P L, Mao J C, Kenney D
出版信息
Appl Microbiol. 1969 Aug;18(2):159-65. doi: 10.1128/am.18.2.159-165.1969.
Abstract
The effect of esterification at the 2'-position of desosamine on the antibacterial activity of erythromycin was investigated by determining the bacteriostatic and bactericidal activities of erythromycin and a number of its 2'-esters on S. aureus and relating these activities to the hydrolysis rates of the esters. These studies, together with comparison of the inhibition of protein synthesis in a cell-free system isolated from S. aureus, lead to the conclusion that 2'-esters of erythromycin are inactive until hydrolyzed. Loss of activity appears to result from inability of erythromycin esters to bind to bacterial ribosomes and thus inhibit synthesis of protein.
摘要
通过测定红霉素及其多种2'-酯对金黄色葡萄球菌的抑菌和杀菌活性，并将这些活性与酯的水解速率相关联，研究了去氧氨基糖2'-位酯化对红霉素抗菌活性的影响。这些研究，再加上对从金黄色葡萄球菌中分离出的无细胞系统中蛋白质合成抑制作用的比较，得出结论：红霉素的2'-酯在水解前无活性。活性丧失似乎是由于红霉素酯无法与细菌核糖体结合，从而抑制蛋白质合成所致。
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