A study on the antioxidant activities of some new benzazole derivatives

Department of Pharmaceutical Chemistry, Ankara University, Engüri, Ankara, Turkey
Acta Biologica Hungarica (Impact Factor: 0.59). 07/2006; 57(2):201-9. DOI: 10.1556/ABiol.57.2006.2.7
Source: PubMed


The in vitro antioxidant properties of some new benzazole derivatives (1-10) such as benzoxazoles, benzimidazoles, and benzothiazoles were determined by their effects on the rat liver microsomal NADPH-dependent lipid peroxidation (LP) level, the scavenging of superoxide anion and the stable radical 2,2-diphenyl-1-picrylhydrazyl (DPPH). Compounds 1, 2, 4 and 6, showed potent scavenging effect on superoxide radical at 10(-3) M. Compound 8, 5-nitro-2-(phenoxymethyl)benzimidazole, strongly inhibited lipid peroxidation at 10(-3) M concentration.

Download full-text


Available from: Ozlem Temiz-Arpaci
  • [Show abstract] [Hide abstract]
    ABSTRACT: Antioxidant effect of 2-methyl-1,3-benzoxazol-6-ol in radical chain oxidation of organic compounds with molecular oxygen was studied. Antiradical activity in the reaction with stable diphenylpicrylhydrazyl radical was examined by photocolorimetry. The kinetic parameters of the reaction of 2-methyl-1,3-benzoxazol-6-ol with peroxy radicals of different natures were determined by volumetric and chemiluminescence methods. A relation was found between the antioxidant activity and electronic structure parameters calculated by quantum-chemical methods. Factors responsible for differences in chemiluminescence in the oxidation of organic substances with different polarities in the presence of the title compound were analyzed.
    No preview · Article · Jan 2011 · Russian Journal of General Chemistry
  • [Show abstract] [Hide abstract]
    ABSTRACT: 2-Benzylbenzothiazoles were easily N-aminated by tosyl hydroxylamine, and the obtained N-amino salts were reacted with ethyl orthoformate to give new derivatives of the pyrazolo[5,1-b][1,3]benzothiazole ring system. Mechanistic considerations suggest that the ring closure reaction proceeds via deprotonation of the N-amino salt followed by electrocyclization to provide the tricyclic ring system. The procedure opens an easy access to variously substituted derivatives of the target ring system.
    No preview · Article · Aug 2008 · Heterocycles
  • Source
    [Show abstract] [Hide abstract]
    ABSTRACT: 3-(4-(Benzo[d]thiazol-2-yl)-1-phenyl-1H-pyrazol-3-yl) phenyl acetate (DPB-5) is a synthetic benzothiazole derivative. In the present study, we revealed that DPB-5 had strong cytotoxicity to induce cell apoptosis, which was mediated by ROS. And DPB-5 was more cytotoxic toward hepatoma cells than toward normal hepatic cells, which was resulted from the greater susceptibility of the malignant cells to ROS. DBP-5 caused massive ROS accumulation and GSH decrease, which lead to MMP disruption, caspase activation and finally induced cell apoptosis. Additionally, rotenone, an inhibitor of mitochondria electron transport system, effectively blocked the ROS elevated effect of DPB-5, which suggested that DPB-5-induced ROS generated from the mitochondria. Further studies showed that DPB-5-induced cell apoptosis through caspases-cascade, but failed to activate caspase-9. Hence, we concluded that DPB-5-induced Hep G2 cells apoptosis via a ROS-mediated pathway which was caspase-dependent but did not rely on caspase-9.
    Preview · Article · Dec 2009 · Chemico-biological interactions
Show more