Effect of varying the 4"-position of arbekacin derivatives on antibacterial activity against MRSA and Pseudomonas aeruginosa

被引：10
作者：
Hiraiwa, Yukiko
Minowa, Nobuto [1 ]
Usui, Takayuki
Akiyama, Yoshihisa
Maebashi, Kazunori
Ikeda, Daishiro
机构：
[1] Meiji Seika Kaisha Ltd, Pharmaceut Res Ctr, Kohoku Ku, Yokosuka, Kanagawa 2228567, Japan
[2] Microbial Chem Res Ctr, Tokyo 1410021, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 22期
关键词：
aminoglycoside; methicillin-resistant; Staphylococcus aureus; Pseudomonas aeruginosa; efflux pump; aminoglycoside-modifying enzyme;
D O I：
10.1016/j.bmcl.2007.08.059
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
4 ''-Deoxy-4 ''-episubstituted arbekacin derivatives and 4 ''-epi-5-deoxy-5-episubstituted arbekacin derivatives were designed and synthesized. Arbekacin and 4 ''-epiarbekacin both displayed the same antibacterial activity against Staphylococcus aureus (including methicillin-resistant S. aureus (MRSA)) and Pseudomonas aeruginosa. The 4 ''-epi-5-deoxy-5-episubstituted arbekacin derivatives showed potent antibacterial activity. Among them, the antibacterial activity of 5,4 ''-diepiarbekacin was superior to that of arbekacin or 5-episubstituted arbekacin against Gram-positive and Gram-negative bacteria. The 6 '-N-methyl derivative of the 5,4 ''-diepiarbekacin was effective against P. aeruginosa expressing an aminoglycoside-modifying enzyme AAC(6 ')-Ib. (C) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：6369 / 6372
页数：4
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