Antiradical and NO-Inhibiting activities of β-hydroxy(ethoxy) derivatives of nitrous heterocycles

The antiradical and NO-inhibiting activities of β-hydroxy(ethoxy) derivatives of nitrous heterocycles (3-hydroxypyridine, 5-hydroxybenzimodazole, and 6-hydroxy(alkoxy)-benzothiazole) have been studied. The antiradical activity has been studied using a homogeneous hydrophilic chemiluminescent system, and the quenching constants (K i ) have been determined. For the most reactive compound, 4-methylthiobenzimidazolyl-3-hydroxypyridine, K i = 4.5 × 105 M−1. The NO-inhibiting activity was estimated on a model of the endotoxin shock of experimental animals using a spin trap of nitric oxide radicals based on complexes of iron with sodium diethyldithiocarbamate. It was found that the compounds at doses of 0.25–1 mmol/kg have both the inhibitory and stimulating action on the production of nitric oxide in the liver of animals. The results obtained suggest that some derivatives of nitrous heterocycles can be used as effective antioxidant preparations.