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  Česky / Czech version Čes. slov. Farm. 52, 2003, č. 4, s. 171–175
 
Antioxidative Activity of Pyridoindoles and N-(Alkoxyphenyl)-2-(2-oxo-1-aza-1-cykloalkyl) Acetamides in Biological, Enzymatic, and Chemical Systems 
PAZOURKOVÁ M., LOJEK A.1, ČÍŽM.1, KUBALA L.1, BENEŠ L., FARSA O. 

Ústav chemických léčiv Farmaceutické fakulty Veterinární a farmaceutické univerzity, Brno 1 Biofyzikální ústav AV ČR, Brno
 


Summary:

       The luminol-enhanced chemiluminiscence method was used to investigate the antioxidative activity of N-(alkoxyphenyl)-2-(2-oxo-1-aza-1-cykloalkyl) acetamides studied as potential cognitive enhancers and stobadine acylderivatives which form prodrugs with increased lipophilicity. The effect on the production of reactive oxygen metabolites by activated leukocytes was studied in vitro. Furthermore, the total radical-trapping antioxidant parameter was evaluated as the peroxyl radical-trapping capacity and the scavenging effect on the superoxide anion radical (generated by the enzymatic system hypoxanthine/xanthine oxidase) and on the hydroxyl radical (produced in Fenton reaction) were studied. The antioxidative properties of the tested substances were compared with that of stobadine dihydrochloride. Only stobadine and its butyrylderivative have been demonstrated to possess free radical scavenging activity in all systems. Cinnamoylstobadine inhibited only the leukocyte chemiluminiscence activity. The potential cognitive enhancers did not show any antioxidant activity.

        Key words: pyridoindoles – cycloalkylacetamides – chemiluminiscence – antioxidative activity
       

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