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, cilt.30, sa.2, ss.173-179, 2015 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 30 Sayı: 2
  • Basım Tarihi: 2015
  • Doi Numarası: 10.3109/14756366.2014.899593
  • Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.173-179
  • Anahtar Kelimeler: 1H-benzimidazole-5-carboxamidines, 1H-benzimidazole-5-carboxylic acid, 1H-benzimidazole-5-sulfonamide, antistaphylococcal activity, MRSA, POLAR SURFACE-AREA, ANTIMICROBIAL ACTIVITY, BENZIMIDAZOLES, NUCLEOSIDES, DERIVATIVES
  • Ankara Üniversitesi Adresli: Evet

Özet

A series of new 2-[4-(3,4-dimethoxyphenoxy) phenyl]-1, N-disubstituted-1H-benzimidazole-5carboxamidines (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 3.12 mu g/mL.