Abstract
A number of benzimidazole compounds namely, N-(4-(1H-benzimidazol-2-yl)phenyl)-4-(1H-benzimidazol-2- yl)-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%).
Keywords: Benzimidazole, Synthesis, Antimicrobial, Antioxidant
Letters in Drug Design & Discovery
Title: Synthesis, Antimicrobial and Antioxidant Activities of Some Benzimidazole Derivatives
Volume: 6 Issue: 5
Author(s): Canan Kus, Gulgun Ayhan-K1lc1gil, Meral Tuncbilek, Nurten Altanlar, Tulay Coban, Benay Can-Eke and Mumtaz Iscan
Affiliation:
Keywords: Benzimidazole, Synthesis, Antimicrobial, Antioxidant
Abstract: A number of benzimidazole compounds namely, N-(4-(1H-benzimidazol-2-yl)phenyl)-4-(1H-benzimidazol-2- yl)-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%).
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Kus Canan, Ayhan-K1lc1gil Gulgun, Tuncbilek Meral, Altanlar Nurten, Coban Tulay, Can-Eke Benay and Iscan Mumtaz, Synthesis, Antimicrobial and Antioxidant Activities of Some Benzimidazole Derivatives, Letters in Drug Design & Discovery 2009; 6 (5) . https://dx.doi.org/10.2174/1570180810906050374
DOI https://dx.doi.org/10.2174/1570180810906050374 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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