氨基糖苷类抗生素的构效关系：羟基和氨基的作用
Structure-activity relationships among the aminoglycoside antibiotics: role of hydroxyl and amino groups.
作者信息
Benveniste R, Davies J
出版信息
Antimicrob Agents Chemother. 1973 Oct;4(4):402-9. doi: 10.1128/AAC.4.4.402.
Abstract
The close structural similarity of several of the deoxystreptamine-containing aminoglycoside antibiotics (gentamicins, neomycins, kanamycins, tobramycin) and the recent isolation of enzymatically N-acetylated aminoglycosides have permitted a systematic comparison of the structure-activity relationships in this group of antibiotics. The number and location of amino groups on the hexoses and the site of attachment of the other rings to deoxystreptamine have been shown to exert a profound effect on the ability of these compounds to inhibit or to cause misreading of polypeptide synthesis in vitro. The conclusions allow certain predictions to be made concerning the interaction of these compounds with the bacterial ribosome.
摘要
几种含脱氧链霉胺的氨基糖苷类抗生素（庆大霉素、新霉素、卡那霉素、妥布霉素）在结构上极为相似，且近期分离出了经酶促N - 乙酰化的氨基糖苷类物质，这使得对该类抗生素的构效关系能够进行系统比较。已表明己糖上氨基的数量和位置以及其他环与脱氧链霉胺的连接位点，对这些化合物在体外抑制或导致多肽合成错读的能力有深远影响。这些结论有助于对这些化合物与细菌核糖体的相互作用做出某些预测。
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