Synthesis and biological evaluation of novel luteolin derivatives as antibacterial agents.
A series of luteolin derivatives 2-20 were prepared, 3-20 of which were first reported. The chemical structures of these compounds were confirmed by means of 1H NMR, ESI-MS and elemental analyses. The compounds were assayed for antibacterial (Bacillus subtilis, Staphylococcus aureus, Pseudomonas fluorescens and Escherichia coli) activities by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl trtrazolium bromide) method. Among the compounds tested, most of them displayed significant activity against the tested strains, and 2-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-hydroxy-7-(2-(3-morpholinopropylamino)ethoxy)-4H-chromen-4-one (17) showed the most favorable antibacterial activity in vitro with MICs of 1.562, 3.125, 3.125, and 6.25 microg/mL against B. subtilis, S. aureus, P. fluorescens and E. coli, respectively. Structure-activity relationships (SAR) were also discussed based on the obtained experimental data.
Lv
Peng-Cheng
PC
Institute of Functional Biomolecules, State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, People's Republic of China.
Li
Huan-Qiu
HQ
Xue
Jia-Yu
JY
Shi
Lei
L
Zhu
Hai-Liang
HL
D000900:Anti-Bacterial Agents / Q000737:chemistry*; D001412:Bacillus subtilis / Q000187:drug effects; D004926:Escherichia coli / Q000187:drug effects; D047311:Luteolin / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D011551:Pseudomonas fluorescens / Q000187:drug effects; D013057:Spectrum Analysis; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D047311:Luteolin