Synthesis and antibacterial activity of C2-fluoro, C6-carbamate ketolides, and their C9-oximes

Bioorg Med Chem Lett. 2005 Feb 15;15(4):883-7. doi: 10.1016/j.bmcl.2004.12.067.

Abstract

Novel C6-carbamate ketolides with C2-fluorination and C9-oximation have been synthesized. The best compounds in this series displayed MIC values of 0.03-0.12 microg/mL against streptococci containing erm and mef resistance determinants and 2-4 microg/mL against Haemophilus influenzae. Several compounds also showed measurable activity against erm(B)-containing enterococci with MIC values of 2-8 microg/mL. In vivo activity was adversely affected by fluorination, possibly as a result of increased serum protein binding.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology
  • Ketolides / chemical synthesis*
  • Ketolides / pharmacology
  • Microbial Sensitivity Tests
  • Oximes / chemical synthesis
  • Oximes / pharmacology
  • Streptococcus / drug effects
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Ketolides
  • Oximes