RESUMO
Antioxidant and radical scavenging properties of a series of 2-[4-(substituted piperazin-/piperidin-1-ylcarbonyl)phenyl]-1H-benzimidazole derivatives were examined. Free radical scavenging properties of compounds 11-30 and 33 were evaluated for the stable free radical 2,2-diphenyl-1-picrylhydrazyl (DPPH) and superoxide anion radical. In addition the inhibitory effects on the NADPH-dependent lipid peroxidation levels were determined by measuring the formation of 2-thiobarbituric acid reactive substances (TBARS) using rat liver microsomes. Compound 33 which has a p-fluorobenzyl substitutent at position 1 exhibited the strongest inhibition (83%) of lipid peroxidation at a concentration of 10(-3) M, while the nonsubstituted analogue 13 caused 57% inhibition. This result is fairly consistent with the antimicrobial activity results against both Staphylococcus aureus and Candida albicans.
Assuntos
Antifúngicos/farmacologia , Antioxidantes/farmacologia , Benzimidazóis/farmacologia , Sequestradores de Radicais Livres/farmacologia , Superóxidos/farmacologia , Animais , Compostos de Bifenilo/farmacologia , Hidroxitolueno Butilado/farmacologia , Peroxidação de Lipídeos/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , NADP/metabolismo , Picratos/farmacologia , Ratos , Ratos Wistar , Superóxidos/metabolismoRESUMO
In this study, we report the synthesis and antimicrobial evaluation of several new 4-(1H-benzimidazol-2-yl)benzamides (11-30) and 5-chloro-1-(p-fluorobenzyl)-2-{4-[(4-methylpiperazin-1-yl)carbonyl]phenyl}-1H-benzimidazole (33). Compound 20 exhibited the best antibacterial activity with MIC value of 6.25 microg/mL against Staphylococcus aureus and methicillin-resistant Staphylococcus aureus (MRSA). Significant antifungal activities were obtained with the compounds 13, 14, 18, 19, and 33 with MIC values of 3.12 microg/mL which are close to fluconazole.
