In vitro and intracellular activities of peptide deformylase inhibitor GSK1322322 against Legionella pneumophila isolates

Antimicrob Agents Chemother. 2015 Jan;59(1):707-10. doi: 10.1128/AAC.04006-14. Epub 2014 Oct 27.

Abstract

GSK1322322, a novel peptide deformylase inhibitor currently in development as an oral and intravenous agent for the treatment of hospitalized community-acquired bacterial pneumonia, showed poor in vitro activity against a panel of 50 Legionella pneumophila strains, with MICs ranging from 1 to 16 μg/ml and an MIC90 of 16 μg/ml, but very potent intracellular activity, with the minimum extracellular concentrations capable of inhibiting intracellular proliferation (MIECs) ranging from 0.12 to 2 μg/ml and 98% of the strains being inhibited by concentrations of ≤ 1 μg/ml.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / pharmacology*
  • Anti-Bacterial Agents / therapeutic use
  • Azithromycin / pharmacology
  • Bridged Bicyclo Compounds, Heterocyclic / pharmacology*
  • Bridged Bicyclo Compounds, Heterocyclic / therapeutic use
  • Humans
  • Hydroxamic Acids / pharmacology*
  • Hydroxamic Acids / therapeutic use
  • Legionella pneumophila / drug effects*
  • Legionnaires' Disease / drug therapy
  • Levofloxacin / pharmacology
  • Microbial Sensitivity Tests

Substances

  • Anti-Bacterial Agents
  • Bridged Bicyclo Compounds, Heterocyclic
  • GSK1322322
  • Hydroxamic Acids
  • Levofloxacin
  • Azithromycin