Synthesis, Antimicrobial and Antioxidant Activities of Some Benzimidazole Derivatives

KUŞ C., KILCIGİL G., TUNÇBİLEK M., ALTANLAR N., Coban T., EKE B., ...More

LETTERS IN DRUG DESIGN & DISCOVERY, vol.6, no.5, pp.374-379, 2009 (SCI-Expanded) identifier identifier

  • Publication Type: Article / Article
  • Volume: 6 Issue: 5
  • Publication Date: 2009
  • Doi Number: 10.2174/1570180810906050374
  • Journal Name: LETTERS IN DRUG DESIGN & DISCOVERY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.374-379
  • Keywords: Benzimidazole, Synthesis, Antimicrobial, Antioxidant, LIPID-PEROXIDATION, INDOLE
  • Ankara University Affiliated: Yes

Abstract

A number of benzimidazole compounds namely, N-(4-(1H-benzimidazol-2-yl) phenyl)-4-(1H-benzimidazol-2yl)-benzamide derivatives (8-10) and N-(3- or 4-(1H-benzimidazol-2-yl) phenyl)-2-phenyl-1H-benzimidazole-5-carboxamide derivatives (18-21) were synthesized and antibacterial and antioxidant activities were evaluated. Antibacterial activities of 9, 10, 18, and 20 against MRSA-isolate are equal to ampicillin. Compounds 18, 19, and 21 displayed better antifungal activities against Candida albicans. Antioxidant properties were evaluated by several methods, such as inhibition of lipid peroxidation, superoxide anion production, and DPPH stable free radical, and also their effects on hepatic cytochrome P450 (CYP) dependent ethoxyresorufin O-deethylase (EROD) enzyme were determined in rats in vitro. Compounds 18 and 20 had strong scavenger effect on superoxide anion (90%, and 99%, respectively) at 10(-3) M concentration. Compound 19 showed significant inhibition on EROD activity with 98%, which is better than that of caffeine being a specific inhibitor of EROD activity (85%).