Thiazolidione derivatives as novel antibiofilm agents: Design, synthesis, biological evaluation, and structure-activity relationships

被引：79

作者：

Pan, Bin ^{[1
]}

Huang, Renzheng ^{[2
,3
,4
]}

Zheng, Likang ^{[1
]}

Chen, Chen ^{[1
]}

Han, Shiqing ^{[1
]}

Qu, Di ^{[2
,3
,4
]}

Zhu, Mingli ^{[1
]}

Wei, Ping ^{[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, Shanghai Med Sch, 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

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 46卷 / 03期

基金：

中国国家自然科学基金;

关键词：

Thiazolidione; Staphylococcus epidermidis; Antibiofilm activity; Inhibitors; INHIBITORS; BIOFILMS; 5-ARYLIDENE-2,4-THIAZOLIDINEDIONES;

D O I：

10.1016/j.ejmech.2010.12.014

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Rational designed novel thiazolidiones were synthesized and evaluated for antibiofilm activity. The active derivatives were not only potent inhibitors of Staphylococcus epidermidis biofilm growth but also efficient antibacterial agents. 3f showed 4-fold higher activity (6.25 mu M) in the biofilms dispersal assay and significantly higher antibacterial activity (MIC 3.125 mu M) in comparison to the 3-(5-((6- (ethoxycarbonyl)-5-(benzo[1,3]dioxol-5-yl)-3-oxo-7-phenyl- thiazolo[3,2-a]pyrimidin-2(5H)-ylidene)methyl) furan-2-yl)benzoic acid (1). (C) 2010 Elsevier Masson SAS. All rights reserved.

引用

页码：819 / 824

页数：6

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