Novel pleuromutilin derivatives with excellent antibacterial activity against Staphylococcus aureus

Chem Biol Drug Des. 2009 Jun;73(6):655-60. doi: 10.1111/j.1747-0285.2009.00821.x.

Abstract

Ten novel pleuromutilin derivatives with thioether moiety and heterocyclic carboxamide or chloroformate group in the side chain were synthesized and confirmed by (1)H NMR, IR and HRMS. The results of the antibacterial activity showed that the title compounds had excellent antibacterial activity against Staphylococcus aureus, among which the MIC of 5f reached 0.03125 microg/mL.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / pharmacology
  • Diterpenes / chemistry
  • Diterpenes / pharmacology
  • Microbial Sensitivity Tests
  • Pleuromutilins
  • Polycyclic Compounds / chemical synthesis
  • Polycyclic Compounds / chemistry*
  • Polycyclic Compounds / pharmacology
  • Pyrazoles / chemical synthesis
  • Pyrazoles / chemistry*
  • Pyrazoles / pharmacology
  • Staphylococcus aureus / drug effects*

Substances

  • Anti-Bacterial Agents
  • Diterpenes
  • Polycyclic Compounds
  • Pyrazoles
  • mutilin 14-O-(1-(1-methyl-4-nitro-3-propyl-1H-pyrazolecarboxamide)-2-methylpropane-2-yl)thioacetate