Design, synthesis, and biological evaluation of chrysin derivatives as potential FabH inhibitors

New series of chrysin derivatives were designed and synthesized by introducing different substituted piperazines at C-7 position. Their inhibitory effects on FabH were evaluated using two Gram-negative bacterial strains, Escherichia coli and Pseudomonas aeruginosa, and two Gram-positive bacterial strains, Bacillus subtilis and Staphylococcus aureus. Most of these compounds exhibited a dramatic increase in inhibitory potency, compared with the control positive drugs

Hong-Xia Li

2016

Scholarcy highlights

  • New series of chrysin derivatives were designed and synthesized by introducing different substituted piperazines at C-7 position. Their inhibitory effects on FabH were evaluated using two Gram-negative bacterial strains, Escherichia coli and Pseudomonas aeruginosa, and two Gram-positive bacterial strains, Bacillus subtilis and Staphylococcus aureus. Most of these compounds exhibited a dramatic increase in inhibitory potency, compared with the control positive drugs
  • Compound 4s exhibited the most potent inhibitory activity with IC50 values of 5.78 ± 0.24 μm inhibiting E. coli FabH and potent antibacterial activity against S. aureus and E. coli with MIC of 1.25 ± 0.01, 1.15 ± 0.12 μg/mL, respectively, comparing to the control positive drugs penicillin G
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