Thiazolidione derivatives as novel antibiofilm agents: design, synthesis, biological evaluation, and structure-activity relationships.
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).
College of Biotechnology and Pharmaceutical Engineering, Nanjing University of Technology, Nanjing 210009, China.
Bin
B
Pan
Renzheng
R
Huang
Likang
L
Zheng
Chen
C
Chen
Shiqing
S
Han
Di
D
Qu
Mingli
M
Zhu
Ping
P
Wei
D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D018441:Biofilms / Q000187:drug effects*; D006801:Humans; D008826:Microbial Sensitivity Tests; D013203:Staphylococcal Infections / Q000188:drug therapy; D013212:Staphylococcus epidermidis / Q000187:drug effects*; D013329:Structure-Activity Relationship; D053778:Thiazolidines / Q000737:chemistry* / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D053778:Thiazolidines