In vitro and in vivo antibacterial evaluation of DRF 8417, a new oxazolidinone

J Antimicrob Chemother. 2007 Jul;60(1):159-61. doi: 10.1093/jac/dkm116. Epub 2007 Apr 21.

Abstract

Objectives and methods: DRF 8417, a novel oxazolidinone, has been evaluated against Gram-positive and fastidious Gram-negative bacteria. In vitro activity of DRF 8417 was determined by broth microdilution method and in vivo efficacy studies were carried out in different murine systemic infection models.

Results: DRF 8417 exhibited potent activity against Gram-positive pathogens with MIC(50) and MIC(90) values ranging from 0.06 to 1 mg/L. MICs against Haemophilus influenzae and Moraxella catarrhalis were one to two dilutions lower than those of linezolid. The in vivo efficacy, by oral route, in different susceptible and resistant Gram-positive systemic bacterial infection models ranged from 2.0 to 2.9 mg/kg.

Conclusions: These studies displayed the excellent in vitro and in vivo activity of DRF 8417 against Gram-positive pathogens and lower MICs when compared with linezolid against H. influenzae and M. catarrhalis.

MeSH terms

  • Animals
  • Anti-Infective Agents* / chemistry
  • Anti-Infective Agents* / pharmacology
  • Anti-Infective Agents* / therapeutic use
  • Disease Models, Animal
  • Female
  • Gram-Negative Bacterial Infections / drug therapy*
  • Gram-Negative Bacterial Infections / microbiology
  • Gram-Positive Bacterial Infections / drug therapy*
  • Gram-Positive Bacterial Infections / microbiology
  • Gram-Positive Cocci / drug effects*
  • Haemophilus Infections / drug therapy
  • Haemophilus Infections / microbiology
  • Haemophilus influenzae / drug effects*
  • Haemophilus influenzae / enzymology
  • Humans
  • Male
  • Mice
  • Microbial Sensitivity Tests
  • Moraxella catarrhalis / drug effects*
  • Moraxellaceae Infections / drug therapy
  • Moraxellaceae Infections / microbiology
  • Oxazolidinones* / chemistry
  • Oxazolidinones* / pharmacology
  • Oxazolidinones* / therapeutic use
  • Specific Pathogen-Free Organisms
  • Treatment Outcome
  • beta-Lactam Resistance
  • beta-Lactamases / metabolism

Substances

  • Anti-Infective Agents
  • Oxazolidinones
  • beta-Lactamases