Synthesis and evaluation of galactofuranosyl N,N-dialkyl sulfenamides and sulfonamides as antimycobacterial agents

被引:42
作者
Owen, David J. [1 ]
Davis, Chris B. [1 ]
Hartnell, Regan D. [1 ]
Madge, Paul D. [1 ]
Thomson, Robin J. [1 ]
Chong, Andrew K. J. [1 ]
Coppel, Ross L. [1 ]
von Itzstein, Mark [1 ]
机构
[1] Monash Univ, Dept Microbiol, Clayton, Vic 3168, Australia
基金
英国医学研究理事会; 澳大利亚研究理事会;
关键词
galactofuranosyl; sulfenamide; sulfonamide; mycobacterium; antibacterial; inhibition;
D O I
10.1016/j.bmcl.2007.01.068
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The recent emergence of clinically oppressive superbugs, some with resistance to nearly all frontline drug therapies, has challenged our ability to combat such infectious organisms as Mycobacterium tuberculosis, the causative agent of tuberculosis (TB). Our medicinal chemistry program targeting this pathogen has identified several potent galactofuranose-based in vitro inhibitors of mycobacterial growth. The most potent compound, the Galf N,N-didecyl sulfenamide 8d, displayed anti-mycobacterial activity (MIC) of 1 mu g/mL in a cell based assay against a representative strain of Mycobacterium smegmatis. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2274 / 2277
页数:4
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