Probing the functional requirements of the L-haba side-chain of amikacin-synthesis, 16S A-site rRNA binding, and antibacterial activity
Probing the functional requirements of the L-haba side-chain of amikacin-synthesis, 16S A-site rRNA binding, and antibacterial activity
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DOI：
10.1016/s0040-4020(02)01625-3
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发表时间：
2003-02-10
期刊：
影响因子：
2.1
通讯作者：
Swayze, EE
中科院分区：
文献类型：
--
作者：
Hanessian, S;Kornienko, A;Swayze, EE
将阿米卡星中的1-氨基与多种2-羟基氨基甲酸进行酰化反应，探讨酰化反应对核糖体结合和抗菌活性的影响。阿米卡星(8a)的N-羟基脲类似物(8a)中的2-S羟基碳被N-羟基取代，在体外对金黄色葡萄球菌和大肠杆菌具有同等的抗菌活性。类似的妥布霉素变异体9比阿米卡星更有活性。(C)2003爱思唯尔科学有限公司。保留所有权利。
The 1-amino group in amikacin was acylated with a variety of 2-hydroxy aminocarboxylic acids to probe the effect of acylation on ribosomal binding and antibacterial activity. The N-hydroxy urea analogue of amikacin (8a) in which the 2-S-hydroxyl-bearing carbon was replaced by an N-OH group was equally active against S. aureus and E. coli in vitro. The analogous tobramycin variant 9 was more active than amikacin. (C) 2003 Elsevier Science Ltd. All rights reserved.