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某些含1-苯并咪唑的亚胺的抗氧化活性评估

Evaluation of the Antioxidant Activity of Some Imines Containing 1-Benzimidazoles.

作者信息

Başaran Rahman, Kılcıgil Gülgün, Eke Benay

机构信息

University of Leeds, School of Chemistry, Leeds, United Kingdom.

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

出版信息

Turk J Pharm Sci. 2020 Dec 23;17(6):626-630. doi: 10.4274/tjps.galenos.2019.05914.

Abstract

OBJECTIVES

The antioxidant properties of some 2-(2-phenyl)-1-benzo(d)imidazol-1-yl)-N'-(arylmethylene) acetohydrazide derivatives (1-12) were investigated in this study.

MATERIALS AND METHODS

The antioxidant activity of compounds 1-12 was explored by determination of rat liver microsomal nicotinamideadenine dinucleotide phosphate dependent inhibition on lipid peroxidation (LPO) levels and microsomal ethoxyresorufin O-deethylase (EROD) activity.

RESULTS

All synthesised compounds had LPO inhibitory activity (15-57%) except compound 6, which contains a thiophene ring. Almost all the compounds displayed slightly inhibitory activity (2-20%) on EROD.

CONCLUSION

The most active compound, 3 bearing a p-bromophenyl substituent at the second position of the benzimidazole ring, caused 57% inhibition of LPO level, while butylated hydroxytoluene showed 65% inhibition. None of the synthesised compounds had a marked inhibitory effect on EROD activity.

摘要

目的

本研究对一些2-(2-苯基)-1-苯并(d)咪唑-1-基)-N'-(芳基亚甲基)乙酰肼衍生物(1-12)的抗氧化性能进行了研究。

材料与方法

通过测定大鼠肝微粒体烟酰胺腺嘌呤二核苷酸磷酸依赖性对脂质过氧化(LPO)水平的抑制作用以及微粒体乙氧基异吩恶唑酮O-脱乙基酶(EROD)活性,探究化合物1-12的抗氧化活性。

结果

除含有噻吩环的化合物6外,所有合成化合物均具有LPO抑制活性(15-57%)。几乎所有化合物对EROD均表现出轻微抑制活性(2-20%)。

结论

活性最高的化合物3在苯并咪唑环的第二位带有对溴苯基取代基,对LPO水平的抑制率为57%,而丁基化羟基甲苯的抑制率为65%。所有合成化合物对EROD活性均无明显抑制作用。

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