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

GÖKER A. H., ÖZDEN M. S., Yildiz S., Boykin D. W.

European Journal of Medicinal Chemistry, vol.40, no.10, pp.1062-1069, 2005 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 40 Issue: 10
  • Publication Date: 2005
  • Doi Number: 10.1016/j.ejmech.2005.05.002
  • Journal Name: European Journal of Medicinal Chemistry
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.1062-1069
  • Keywords: 1H-benzimidazole-carboxamidines, methicilline resistant S. aureus, antibacterial activity, RESISTANT STAPHYLOCOCCUS-AUREUS, METHICILLIN
  • Lokman Hekim University Affiliated: No


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 μg/ml. © 2005 Elsevier SAS. All rights reserved.