Rahman Başaran1, Gülgün Kılcıgil2, Benay Eke3. 1. University of Leeds, School of Chemistry, Leeds, United Kingdom. 2. Ankara University Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ankara, Turkey. 3. Ankara University Faculty of Pharmacy, Department of Pharmaceutical Toxicology, Ankara, Turkey.
Abstract
OBJECTIVES: The in vitro antioxidant properties of some 2-(2-phenyl)-1H-benzo(d)imidazol-1-yl)-N'-(arylmethylene) acetohydrazide derivatives (1-12) were investigated in this study. MATERIALS AND METHODS: The in vitro 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.
OBJECTIVES: The in vitro antioxidant properties of some 2-(2-phenyl)-1H-benzo(d)imidazol-1-yl)-N'-(arylmethylene) acetohydrazide derivatives (1-12) were investigated in this study. MATERIALS AND METHODS: The in vitro 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.
Authors: H Nakano; T Inoue; N Kawasaki; H Miyataka; H Matsumoto; T Taguchi; N Inagaki; H Nagai; T Satoh Journal: Bioorg Med Chem Date: 2000-02 Impact factor: 3.641