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Bioorg Med Chem ; 17(22): 7823-30, 2009 Nov 15.
Artículo en Inglés | MEDLINE | ID: mdl-19819150

RESUMEN

A series of benzazolone compounds were synthesized utilizing benzoxazolinonic and benzothiazolinonic heterocycles as the building unit. The antioxidant activity of these compounds was determined by inhibition of lipid peroxidation. The oxidation of LDL was induced in the presence of CuSO(4) or 2,2'-azobis(2-amidinopropane) dihydrochloride (AAPH). The protective action of these compounds against the cytotoxicity was evaluated with lactate dehydrogenase (LDH) activity in bovine aortic endothelial cells (BAECs) and cellular vitality by measuring mitochondrial activity in the presence of MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide). The best antioxidant activities were observed for phenolic compounds 13 and 14b with ratio R=2.5, 3.2 (5microM). Both of these test substances increased the cell viability significantly as indicated by MTT assay and LDH release assay.


Asunto(s)
Antioxidantes/farmacología , Benzoxazoles/farmacología , Lipoproteínas LDL/metabolismo , Tiazoles/farmacología , Animales , Antioxidantes/síntesis química , Antioxidantes/química , Aorta/citología , Aorta/metabolismo , Aorta/patología , Benzoxazoles/síntesis química , Benzoxazoles/química , Bioensayo , Bovinos , Supervivencia Celular/efectos de los fármacos , Supervivencia Celular/fisiología , Células Endoteliales/efectos de los fármacos , Células Endoteliales/metabolismo , L-Lactato Deshidrogenasa/metabolismo , Oxidación-Reducción/efectos de los fármacos , Tiazoles/síntesis química , Tiazoles/metabolismo
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