Synthesis and potent antistaphylococcal activity of some new 2-[4-(3,4-dimethoxyphenoxy)phenyl]-1,N-disubstituted-1H-benzimidazole-5-carboxamidines


Püsküllü M. O. , YILDIZ S. , DUYDU Y., ÜSTÜNDAĞ A., GÖKER A. H.

Journal of Enzyme Inhibition and Medicinal Chemistry, vol.30, no.2, pp.173-179, 2015 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 30 Issue: 2
  • Publication Date: 2015
  • Doi Number: 10.3109/14756366.2014.899593
  • Title of Journal : Journal of Enzyme Inhibition and Medicinal Chemistry
  • Page Numbers: pp.173-179
  • Keywords: 1H-benzimidazole-5-carboxamidines, 1H-benzimidazole-5-carboxylic acid, 1H-benzimidazole-5-sulfonamide, antistaphylococcal activity, MRSA, POLAR SURFACE-AREA, ANTIMICROBIAL ACTIVITY, BENZIMIDAZOLES, NUCLEOSIDES, DERIVATIVES

Abstract

© 2014 Informa UK Ltd. All rights reserved: reproduction in whole or part not permitted.A series of new 2-[4-(3,4-dimethoxyphenoxy)phenyl]-1,N-disubstituted-1H-benzimidazole-5-carboxamidines (23-33) have been synthesized and evaluated for their potential antistaphylococcal activity. Cytotoxic effects of the compounds were investigated by the neutral red uptake (NRU) cytotoxicity test. Most of the compounds exhibited good MICs values against Staphylococcus aureus and methicillin-resistant S. aureus (MRSA). Compound 28 with N-cyclohexylcarboxamidine group at the 5-position was found to be the most potent agent, with the MIC value of 3.12g/mL.