期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 45, 期 9, 页码 4358-4364出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.05.033
关键词
FabH; Inhibitor; Antibacterial; Structure-activity relationship; Schiff base
资金
- Jiangsu National Science Foundation [BK2009239]
- Anhui National Science Foundation [070416274X]
Twenty new Schiff bases were synthesized by reacting 5-fluoro-salicylaldehyde and primary amine as potent inhibitors of FabH. These compounds were assayed for antibacterial activity against Escherichia coli, Pseudomonas fluorescence, Bacillus subtilis and Staphylococcus aureus. Compounds with potent antibacterial activities were tested for their E. coli FabH inhibitory activity. (E)-4-fluoro-2-((4-hydroxyphenethylimino)methyl)phenol (10) showed the most potent antibacterial activity with MIC of 1.56-6.25 mu g/mL against the tested bacterial strains and exhibited the most potent E. coli FabH inhibitory activity with IC50 of 2.7 mu M. Docking simulation was performed to position compound 10 into the E. coli FabH active site to determine the probable binding conformation. (C) 2010 Elsevier Masson SAS. All rights reserved.
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