Synthesis, crystal structures, and anti-drug-resistant Staphylococcus aureus activities of novel 4-hydroxycoumarin derivatives

Eur J Pharmacol. 2013 Dec 5;721(1-3):151-7. doi: 10.1016/j.ejphar.2013.09.040. Epub 2013 Sep 25.

Abstract

Four novel 4-hydroxycoumarin derivatives (4-MBH, 3-MBH, 4-MDT and 3-MDT) were successfully synthesized and their structures were verified by single-crystal X-ray crystallography. All target compounds were evaluated for their in vitro antibacterial activity against Staphylococcus aureus (S. aureus ATCC 29213), methicillin-resistant S. aureus (MRSA XJ 75302), vancomycin-intermediate S. aureus (Mu50 ATCC 700699), and USA 300 (Los Angeles County clone, LAC). The minimum inhibitory concentration and time-kill curves were obtained for the test compounds and antibiotics. Among the tested compounds, 3-MBH showed the most potent antibacterial activities.

Keywords: 4-Hydroxycoumarin; Minimum inhibitory concentration; Single crystal; Staphylococcus aureus.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 4-Hydroxycoumarins / chemical synthesis*
  • 4-Hydroxycoumarins / chemistry
  • 4-Hydroxycoumarins / pharmacology*
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Chemistry Techniques, Synthetic
  • Crystallography, X-Ray
  • Drug Resistance, Bacterial / drug effects*
  • Microbial Sensitivity Tests
  • Models, Molecular
  • Molecular Conformation
  • Staphylococcus aureus / drug effects*
  • Structure-Activity Relationship
  • Time Factors

Substances

  • 4-Hydroxycoumarins
  • Anti-Bacterial Agents
  • 4-hydroxycoumarin