Brazilian Journal of Pharmaceutical Sciences (Apr 2020)

Synthesis and antibacterial activity of a series novel 5,7-diisoprenyloxyflavone derivatives

  • Qing-Hao Jin,
  • Zhi-Yang Fu,
  • Ya-Nan Xia,
  • Bing-Yu Liu,
  • Hai-Ying Jiang

DOI
https://doi.org/10.1590/s2175-97901919000417721
Journal volume & issue
Vol. 56

Abstract

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In the present study, a series of novel 5,7-diisoprenyloxyflavone derivatives were designed, synthesized, and evaluated for their antibacterial activity. Most of these compounds displayed significant antibacterial effects against Gram-positive bacteria, especially against strains of multidrug-resistant clinical isolates. Compounds 4c, 4g, 4i, 4j, 4k, 4l, 4n, 4q and 4t showed high levels of antimicrobial activity against Staphylococcus aureus RN4220 with minimum inhibitory concentrations of 4.0-20 µM. Compound 4k showed the most potent activity among these compounds against all multidrug-resistant clinical isolates tested. Unfortunately, none of the compounds were active against Gram-negative bacteria at the doses of 24-164 µM.

Keywords