Design, synthesis, and biological evaluation of a novel series of quercetin diacylglucosides as potent anti-MRSA and anti-VRE agents

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5349-52. doi: 10.1016/j.bmcl.2010.02.060. Epub 2010 Feb 19.


A series of novel quercetin diacylglucosides were designed and first synthesized by Steglich esterification on the basis of MRSA strains inhibiting natural compound A. The in vitro inhibition of different multi-drug resistant bacterial strains and Escherichia coli DNA gyrase B was investigated. In the series, compound 10h was up to 128-fold more potent against vancomycin-resistant enterococci and more effective than A, which represents a promising new candidate as a potent anti-MRSA and anti-VRE agent.

MeSH terms

  • Anti-Bacterial Agents / pharmacology*
  • Drug Design
  • Enterococcus / drug effects*
  • Glucosides / chemistry*
  • Methicillin-Resistant Staphylococcus aureus / drug effects*
  • Microbial Sensitivity Tests
  • Quercetin / chemistry
  • Quercetin / pharmacology*
  • Vancomycin / pharmacology*


  • Anti-Bacterial Agents
  • Glucosides
  • Vancomycin
  • Quercetin