Synthesis and antibacterial activity of C12 des-methyl ketolides

Bioorg Med Chem Lett. 2006 Sep 1;16(17):4692-6. doi: 10.1016/j.bmcl.2006.05.104. Epub 2006 Jun 19.

Abstract

Synthesis of C(12) des-methyl ketolide is developed featuring an intramolecular epoxide formation/elimination process to establish the C(12) stereocenter. These ketolides are potent against several key respiratory pathogens, including erythromycin resistant erm- and mef-containing strains of Streptococcus pneumoniae.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Carbon / chemistry*
  • Gram-Positive Cocci / drug effects
  • Haemophilus influenzae / drug effects
  • Ketolides / chemical synthesis
  • Ketolides / chemistry*
  • Ketolides / pharmacology*
  • Methylation
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Ketolides
  • Carbon