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

被引:3
作者
Zhao, Dan [1 ]
Liu, Huayong [2 ,3 ,4 ]
Zheng, Likang [1 ]
He, Guozhen [1 ]
Qu, Di [2 ,3 ,4 ]
Han, Shiqing [1 ]
机构
[1] Nanjing Univ Technol, Coll Biotechnol & Pharmaceut Engn, Nanjing 210009, Peoples R China
[2] Fudan Univ, Minist Educ, Key Lab Med Mol Virol, Shanghai 200032, Peoples R China
[3] Fudan Univ, Minist Publ Hlth, Inst Med Microbiol, Shanghai 200032, Peoples R China
[4] Fudan Univ, Shanghai Med Sch, Inst Biomed Sci, Shanghai 200032, Peoples R China
基金
中国国家自然科学基金; 国家高技术研究发展计划(863计划);
关键词
4-Thiazolidione; Methicillin-resistant Staphylococcus epidermidis; Methicillin-resistant Staphylococcus aureus; Antibacterial activity; 2-COMPONENT; VANCOMYCIN;
D O I
10.1007/s00044-012-0363-9
中图分类号
R914 [药物化学];
学科分类号
100701 ;
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 mu M). 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:8
相关论文
共 18 条
[1]   The involvement of cell-to-cell signals in the development of a bacterial biofilm [J].
Davies, DG ;
Parsek, MR ;
Pearson, JP ;
Iglewski, BH ;
Costerton, JW ;
Greenberg, EP .
SCIENCE, 1998, 280 (5361) :295-298
[2]  
Fabret C, 1998, J BACTERIOL, V180, P6375
[3]   The emergence of decreased susceptibility to vancomycin in Staphylococcus epidermidis [J].
Garrett, DO ;
Jochimsen, E ;
Murfitt, K ;
Hill, B ;
McAllister, S ;
Nelson, P ;
Spera, RV ;
Sall, RK ;
Tenover, FC ;
Johnston, J ;
Zimmer, B ;
Jarvis, WR .
INFECTION CONTROL AND HOSPITAL EPIDEMIOLOGY, 1999, 20 (03) :167-170
[4]   Staphylococcus and biofilms [J].
Götz, F .
MOLECULAR MICROBIOLOGY, 2002, 43 (06) :1367-1378
[5]   Aminoglycoside antibiotics induce bacterial biofilm formation [J].
Hoffman, LR ;
D'Argenio, DA ;
MacCoss, MJ ;
Zhang, ZY ;
Jones, RA ;
Miller, SI .
NATURE, 2005, 436 (7054) :1171-1175
[6]  
Huebner J, 1999, ANNU REV MED, V50, P223, DOI 10.1146/annurev.med.50.1.223
[7]   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].
Luo, Youfu ;
Ma, Liang ;
Zheng, Hao ;
Chen, Lijuan ;
Li, Rui ;
He, Chunmei ;
Yang, Shengyong ;
Ye, Xia ;
Chen, Zhizhi ;
Li, Zicheng ;
Gao, Yan ;
Han, Jing ;
He, Gu ;
Yang, Li ;
Wei, Yuquan .
JOURNAL OF MEDICINAL CHEMISTRY, 2010, 53 (01) :273-281
[8]   Staphylococcus epidermidis biofilms:: importance and implications [J].
O'Gara, JP ;
Humphreys, H .
JOURNAL OF MEDICAL MICROBIOLOGY, 2001, 50 (07) :582-587
[9]   Thiazolidione derivatives as novel antibiofilm agents: Design, synthesis, biological evaluation, and structure-activity relationships [J].
Pan, Bin ;
Huang, Renzheng ;
Zheng, Likang ;
Chen, Chen ;
Han, Shiqing ;
Qu, Di ;
Zhu, Mingli ;
Wei, Ping .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2011, 46 (03) :819-824
[10]   Design, synthesis, and antibiofilm activity of 2-arylimino-3-aryl-thiazolidine-4-ones [J].
Pan, Bin ;
Huang, Ren-Zheng ;
Han, Shi-Qing ;
Qu, Di ;
Zhu, Ming-Li ;
Wei, Ping ;
Ying, Han-Jie .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2010, 20 (08) :2461-2464