Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06100, Tandogan, Ankara, Turkey.
Z Naturforsch C J Biosci. 2010 Sep-Oct;65(9-10):537-42. doi: 10.1515/znc-2010-9-1002.
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.
研究了一系列 2-[4-(取代哌嗪基/哌啶基甲酰基)苯基]-1H-苯并咪唑衍生物的抗氧化和自由基清除特性。评估了化合物 11-30 和 33 的自由基清除特性,针对稳定自由基 2,2-二苯基-1-苦基肼(DPPH)和超氧阴离子自由基。此外,通过使用大鼠肝微粒体测量 2-硫代巴比妥酸反应性物质(TBARS)的形成来确定对 NADPH 依赖性脂质过氧化水平的抑制作用。在浓度为 10(-3) M 时,具有对位氟苄基取代基的化合物 33 对脂质过氧化的抑制作用最强(83%),而未取代的类似物 13 引起 57%的抑制作用。这一结果与对金黄色葡萄球菌和白色念珠菌的抗菌活性结果相当一致。