Peptidomimetics of efflux pump inhibitors potentiate the activity of levofloxacin in Pseudomonas aeruginosa

Bioorg Med Chem Lett. 2002 Mar 11;12(5):763-6. doi: 10.1016/s0960-894x(02)00006-9.

Abstract

Several classes of peptidomimetics of the efflux pump inhibitor D-ornithine-D-homophenylalanine-3-aminoquinoline (MC-02,595) have been prepared and evaluated for their ability to potentiate the activity of the fluoroquinolone levofloxacin in Pseudomonas aeruginosa. A number of the new analogues were as active or more active than the lead, demonstrating that a peptide backbone is not essential for activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Infective Agents / pharmacology*
  • Biological Transport, Active / drug effects
  • Drug Synergism
  • Levofloxacin*
  • Membrane Transport Modulators*
  • Membrane Transport Proteins / antagonists & inhibitors*
  • Microbial Sensitivity Tests
  • Molecular Mimicry
  • Molecular Structure
  • Ofloxacin / pharmacology*
  • Peptide Fragments / chemical synthesis*
  • Peptide Fragments / chemistry
  • Peptide Fragments / pharmacology*
  • Pseudomonas aeruginosa / drug effects*
  • Pseudomonas aeruginosa / physiology
  • Structure-Activity Relationship

Substances

  • Anti-Infective Agents
  • Membrane Transport Modulators
  • Membrane Transport Proteins
  • Peptide Fragments
  • Levofloxacin
  • Ofloxacin