Synthesis and potent antibacterial activity against MRSA of some novel 1,2-disubstituted-1H-benzimidazole-N-alkylated-5-carboxamidines

Eur J Med Chem. 2005 Oct;40(10):1062-9. doi: 10.1016/j.ejmech.2005.05.002. Epub 2005 Jun 29.

Abstract

A series of 28 novel 1,2-disubstituted-1H-benzimidazole-N-alkylated-5-carboxamidine derivatives were synthesized and evaluated for in vitro antibacterial activities against Staphylococcus aureus and methicillin resistant S. aureus (MRSA) by the tube dilution method. The results showed that compounds 45-46 and 55-57, having 3,4-dichloro substituted phenyl at the position C-2, of N-bulky alkyl substituted benzimidazolecarboxamidines exhibited the greatest activity with MIC values of 1.56-0.39 microg/ml.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkylation
  • Amidines / chemical synthesis
  • Amidines / chemistry*
  • Amidines / pharmacology*
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Benzene / chemistry*
  • Imidazoles / chemistry*
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Methicillin Resistance*
  • Molecular Structure
  • Staphylococcus aureus / drug effects
  • Structure-Activity Relationship

Substances

  • Amidines
  • Anti-Bacterial Agents
  • Imidazoles
  • imidazole
  • Benzene