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噻唑烷二酮衍生物作为新型抗生物膜剂的研究:设计、合成、生物评价及构效关系。

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

机构信息

College of Biotechnology and Pharmaceutical Engineering, Nanjing University of Technology, Nanjing 210009, China.

出版信息

Eur J Med Chem. 2011 Mar;46(3):819-24. doi: 10.1016/j.ejmech.2010.12.014. Epub 2010 Dec 21.

Abstract

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 μM) in the biofilms dispersal assay and significantly higher antibacterial activity (MIC 3.125 μM) 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).

摘要

合理设计的新型噻唑烷二酮被合成并评估其抗生物膜活性。活性衍生物不仅是表皮葡萄球菌生物膜生长的有效抑制剂,也是有效的抗菌剂。在生物膜分散试验中,3f 显示出 4 倍的高活性(6.25 μM),与 3-(5-((6-(乙氧羰基)-5-(苯并[1,3]二氧杂环戊烯-5-基)-3-氧代-7-苯基-噻唑并[3,2-a]嘧啶-2(5H)-基)亚甲基)呋喃-2-基)苯甲酸(1)相比,具有更高的抗菌活性(MIC 3.125 μM)。

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