Dicationic 2-fluorenonylcarbapenems: potent anti-MRS agents with improved solubility and pharmacokinetic properties

Bioorg Med Chem Lett. 1999 Nov 15;9(22):3225-30. doi: 10.1016/s0960-894x(99)00567-3.

Abstract

The synthesis and biological evaluation of a series of dicationic-substituted 2-fluorenonylcarbapenems is described. This class of compounds showed enhanced water solubility while maintaining potent activity against MRS. Introduction of a 1-beta-methyl substituent was found to improve pharmacokinetics.

MeSH terms

  • Animals
  • Carbapenems / pharmacokinetics
  • Carbapenems / pharmacology*
  • Carbapenems / therapeutic use
  • Cations
  • Half-Life
  • Macaca mulatta
  • Methicillin Resistance
  • Mice
  • Microbial Sensitivity Tests
  • Solubility
  • Staphylococcal Infections / drug therapy
  • Staphylococcus aureus / drug effects*

Substances

  • Carbapenems
  • Cations