新型苯并咪唑的合成、抗氧化及自由基清除活性

Synthesis, antioxidant and radical scavenging activities of novel benzimidazoles.

作者信息

Ayhan-Kilcigil Gülgün, Kuş Canan, Coban Tülay, Can-Eke Benay, Ozbey Süheyla, Iscan Mümtaz

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06100 Tandoğan, Ankara, Turkey.

出版信息

J Enzyme Inhib Med Chem. 2005 Oct;20(5):503-14. doi: 10.1080/14756360500287086.

DOI:10.1080/14756360500287086

PMID:16335060

Abstract

The synthesis and antioxidant evaluation of some novel benzimidazole derivatives (10-24) are described. Antioxidant properties of the compounds were investigated employing various in vitro systems viz., microsomal NADPH-dependent inhibition of lipid peroxidation (LP), interaction of 2,2-diphenyl-1-picrylhydrazyl (DPPH) and scavenging of superoxide anion radical. Compounds 12 and 13 showed very good antioxidant capacity and were 17-18-fold more potent than BHT (IC50 2.3 x 10(-4) M) with 1.3 x 10(-5) M and 1.2 x 10(-5) M IC50 values, respectively, by interaction of the stable DPPH free radical.

摘要

描述了一些新型苯并咪唑衍生物（10 - 24）的合成及抗氧化性能评估。采用多种体外系统研究了这些化合物的抗氧化性能，即微粒体NADPH依赖性脂质过氧化抑制（LP）、2,2 - 二苯基 - 1 - 苦基肼（DPPH）相互作用以及超氧阴离子自由基清除。通过稳定的DPPH自由基相互作用，化合物12和13表现出非常好的抗氧化能力，其IC50值分别为1.3×10⁻⁵ M和1.2×10⁻⁵ M，比BHT（IC50 2.3×10⁻⁴ M）强17 - 18倍。