Probing the functional requirements of the L-haba side-chain of amikacin-synthesis, 16S A-site rRNA binding, and antibacterial activity

被引：26

作者：

Hanessian, S

Kornienko, A

Swayze, EE

机构：

[1] Univ Montreal, Dept Chem, Montreal, PQ H3C 3J7, Canada

[2] Ibis Therapeut, Carlsbad, CA 92008 USA

来源：

TETRAHEDRON | 2003年 / 59卷 / 07期

基金：

加拿大自然科学与工程研究理事会;

关键词：

aminoglycoside; hydroxyurea; ribosome; antibacterial activity;

D O I：

10.1016/S0040-4020(02)01625-3

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

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.

引用

页码：995 / 1007

页数：13

共 75 条

[1] COMPARISON OF AMINOGLYCOSIDE ANTIBIOTICS WITH RESPECT TO UPTAKE AND LETHAL ACTIVITY IN ESCHERICHIA-COLI [J].