Synthesis of novel 4-thiazolidione derivatives as antibacterial agents against drug-resistant Staphylococcus epidermidis

被引:0
作者
Dan Zhao
Huayong Liu
Likang Zheng
Guozhen He
Di Qu
Shiqing Han
机构
[1] Nanjing University of Technology,College of Biotechnology and Pharmaceutical Engineering
[2] Institute of Medical Microbiology and Institutes of Biomedical Sciences,Key Laboratory of Medical Molecular Virology of Ministry of Education and Ministry of Public Health
[3] Shanghai Medical School of Fudan University,undefined
来源
Medicinal Chemistry Research | 2013年 / 22卷
关键词
4-Thiazolidione; Methicillin-resistant ; Methicillin-resistant ; Antibacterial activity;
D O I
暂无
中图分类号
学科分类号
摘要
A series of novel substituted 4-thiazolidione derivatives were designed, synthesized, and evaluated in vitro for their antibacterial activities, in comparison with methicillin and ampicillin. Compounds (7d, 7h–k) exhibit good potency in inhibiting the growth of Staphylococcus epidermidis (MIC: 1.57–3.13 μM). Further antibacterial effects of compounds (7d, 7h–k) were investigated using clinical isolates (methicillin-resistant Staphylococcus epidermidis and methicillin-resistant Staphylococcus aureus), in comparison with methicillin and levofloxacin. Compound 7k showed the most potent antibacterial activities among the synthesized compounds.
引用
收藏
页码:3743 / 3750
页数:7
相关论文
共 87 条
[1]  
Davies DG(1998)The involvement of cell-to-cell signals in the development of a bacterial biofilm Science 280 295-298
[2]  
Parsek MR(1998)A two-component signal transduction system essential for growth of J Bacteriol 180 6375-6383
[3]  
Pearson JP(1999): implications for anti-infective therapy Infect Control Hosp Epidemiol 20 167-170
[4]  
Iglewski BH(2002)The emergence of decreased susceptibility to vancomycin in Mol Microbio 43 1367-1378
[5]  
Costerton J(2005)Staphylococcus and biofilms Nature 436 1171-1175
[6]  
Greenberg E(1999)Aminoglycoside antibiotics induce bacterial biofilm formation Annu Rev Med 50 223-236
[7]  
Fabret C(2009)Coagulase-negative Staphylococci: role as pathogens J Med Chem 53 273-281
[8]  
Hoch JA(2001)Discovery of (Z)-5-(4-methoxybenzylidene) thiazolidine-2, 4-dione, a readily available and orally active glitazone for the treatment of concanavalin A-induced acute liver injury of BALB/c mice J Med Microbiol 50 582-587
[9]  
Garrett DO(2010) biofilms: importance and implications Bioorg Med Chem Lett 20 2461-2464
[10]  
Jochimsen E(2011)Design, synthesis, and antibiofilm activity of 2-arylimino-3-aryl-thiazolidine-4-ones Eur J Med Chem 46 819-824