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氨基糖苷类抗生素。2. N,N-二烷基卡那霉素

Aminoglycoside antibiotics. 2. N,N-Dialkylkanamycins.

作者信息

Kumar V, Remers W A

出版信息

J Med Chem. 1979 Apr;22(4):432-6. doi: 10.1021/jm00190a015.

Abstract

N6',N3''-Dialkyl derivatives of kanamycins A and B were prepared regiospecifically from the parent antibiotics. Although the dimethyl and diethyl derivatives of kanamycin A were inactive in standard antibacterial assays, the dimethyl derivative of kanamycin B showed moderate activity, especially against various strains of Pseudomonas aeruginosa. A method for the selective dimethylation of the 3''-amino group of kanamycin A also was developed.

摘要

卡那霉素A和B的N6',N3''-二烷基衍生物是由母体抗生素区域特异性制备的。虽然卡那霉素A的二甲基和二乙基衍生物在标准抗菌试验中无活性,但卡那霉素B的二甲基衍生物显示出中等活性,特别是对各种铜绿假单胞菌菌株。还开发了一种对卡那霉素A的3''-氨基进行选择性二甲基化的方法。

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