Synthesis and antibacterial activity of C-12 pyrazolinyl spiro ketolides

Eur J Med Chem. 2010 Dec;45(12):5943-9. doi: 10.1016/j.ejmech.2010.09.060. Epub 2010 Oct 7.

Abstract

A series of C-12 pyrazolinyl spiro ketolide derivatives were designed and synthesized. The C-12 modifications involved replacing the natural C-12 methyl group in clarithromycin core with different pyrazolinyl spiros via chemical synthesis. Potential anti-bacterial activities against both erythromycin-susceptible and erythromycin-resistant bacteria were reported.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Drug Resistance, Bacterial / drug effects*
  • Haemophilus influenzae / drug effects
  • Ketolides / chemical synthesis
  • Ketolides / chemistry
  • Ketolides / pharmacology*
  • Microbial Sensitivity Tests
  • Molecular Conformation
  • Pyrazoles / chemical synthesis
  • Pyrazoles / chemistry
  • Pyrazoles / pharmacology*
  • Spiro Compounds / chemical synthesis
  • Spiro Compounds / chemistry
  • Spiro Compounds / pharmacology*
  • Staphylococcus / drug effects
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Ketolides
  • Pyrazoles
  • Spiro Compounds