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

Bin Pan; Renzheng Huang; Likang Zheng; Chen Chen; Shiqing Han; Di Qu; Mingli Zhu; Ping Wei

doi:10.1016/j.ejmech.2010.12.014

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

Bin Pan, Renzheng Huang, Likang Zheng, Chen Chen, Shiqing Han, Di Qu, Mingli Zhu, Ping Wei

COLLEGE OF BIOTECHNOLOGY AND PHARMACEUTICAL ENGINEERING

Research output: Contribution to journal › Article › peer-review

83 Scopus citations

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).

Original language	English
Pages (from-to)	819-824
Number of pages	6
Journal	European Journal of Medicinal Chemistry
Volume	46
Issue number	3
DOIs	https://doi.org/10.1016/j.ejmech.2010.12.014
State	Published - Mar 2011

Keywords

Antibiofilm activity
Inhibitors
Staphylococcus epidermidis
Thiazolidione

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10.1016/j.ejmech.2010.12.014

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

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).",

keywords = "Antibiofilm activity, Inhibitors, Staphylococcus epidermidis, Thiazolidione",

author = "Bin Pan and Renzheng Huang and Likang Zheng and Chen Chen and Shiqing Han and Di Qu and Mingli Zhu and Ping Wei",

year = "2011",

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doi = "10.1016/j.ejmech.2010.12.014",

language = "英语",

volume = "46",

pages = "819--824",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

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number = "3",

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TY - JOUR

T1 - Thiazolidione derivatives as novel antibiofilm agents

T2 - Design, synthesis, biological evaluation, and structure-activity relationships

AU - Pan, Bin

AU - Huang, Renzheng

AU - Zheng, Likang

AU - Chen, Chen

AU - Han, Shiqing

AU - Qu, Di

AU - Zhu, Mingli

AU - Wei, Ping

PY - 2011/3

Y1 - 2011/3

N2 - 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).

AB - 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).

KW - Antibiofilm activity

KW - Inhibitors

KW - Staphylococcus epidermidis

KW - Thiazolidione

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U2 - 10.1016/j.ejmech.2010.12.014

DO - 10.1016/j.ejmech.2010.12.014

M3 - 文章

C2 - 21255878

AN - SCOPUS:79951671509

SN - 0223-5234

VL - 46

SP - 819

EP - 824

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

IS - 3

ER -

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

Abstract

Keywords

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