Sato M, Mori Y
J Antibiot (Tokyo). 1979 Apr;32(4):371-8. doi: 10.7164/antibiotics.32.371.
Among the new aminoglycoside antibiotic family for fortimicins, components A, C and D have higher activity compared to their 4-N-deacylated components B and KE. Synthesis and antibacterial activities of 4-N-acyl- and 4-N-alkyl-fortimicin B derivatives are described. 4-N-Acylfortimicin B's, which are relatively unstable in alkaline conditions, were converted to stable 4-N-alkyl derivatives with diborane. The activity is greatly affected by the 4-N-substituents, and the presence of hydrophilic group(s) is necessary to confer activity on the derivatives. 4-N-(2-Aminoethyl)-, 4-N-(4-amino-2-hydroxybutyl)- and 4-N-(2-hydroxy-4-methylaminobutyl)-fortimicin B are the most potent compounds among them.
在新的用于福提霉素的氨基糖苷类抗生素家族中，组分A、C和D与其4-N-脱酰基组分B和KE相比具有更高的活性。本文描述了4-N-酰基-和4-N-烷基-福提米星B衍生物的合成及抗菌活性。在碱性条件下相对不稳定的4-N-酰基福提米星B通过乙硼烷转化为稳定的4-N-烷基衍生物。活性受4-N-取代基的极大影响，并且亲水基团的存在对于赋予衍生物活性是必要的。其中4-N-(2-氨基乙基)-、4-N-(4-氨基-2-羟基丁基)-和4-N-(2-羟基-4-甲基氨基丁基)-福提米星B是最有效的化合物。
