Synthesis and antibacterial activity of novel 4-aryl-[1,2,3]-triazole containing macrolides

Bioorg Med Chem Lett. 2011 Jan 1;21(1):510-3. doi: 10.1016/j.bmcl.2010.10.091. Epub 2010 Oct 25.

Abstract

Two series of novel triazole containing 14-member macrolides having either a cladinose or a 3-pyridyl acetate group at the 3-position of the macrolide ring were synthesized. The in vitro antibacterial activities against S. aureus, S. pneumoniae, S. pyogenes and E. faecalis were determined. Macrolide 7a and the fluoroketolide 1 (CEM-101) were evaluated in vivo in murine systemic infection models. All of the macrolide analogs were less active in vitro and in vivo than the fluoroketolide 1 (CEM-101).

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Bacteremia / drug therapy
  • Macrolides / chemistry*
  • Mice
  • Microbial Sensitivity Tests
  • Streptococcus pneumoniae / drug effects
  • Streptococcus pyogenes / drug effects
  • Triazoles / chemical synthesis
  • Triazoles / chemistry*
  • Triazoles / pharmacology

Substances

  • Anti-Bacterial Agents
  • Macrolides
  • Triazoles