| Title
| - A Novel Series of 2,6,7-Substituted 2,3-Dihydro-1,4-Benzodioxin and2,6,7-Substituted 1,4-Benzodioxin Derivatives as Lipid Peroxidation Inhibitors.Structure−Activity Relationships for High Inhibition of Human Low-DensityLipoprotein Peroxidation
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| Abstract
| - A series of 6- or 7-substituted 2-carboxamido- or 2-(aminomethyl)-1,4-benzodioxin and -2,3-dihydro-1,4-benzodioxin derivatives were synthesized and evaluated to determine the necessarystructural requirements for a high inhibition of human low-density lipoprotein copper-inducedperoxidation. The most active compounds (21, 25, 28, 36, and 37) were found between 5 and>45 times more active than probucol itself. Due to both their potency and their structuralfeatures, compounds 25 and 36 were selected with others for complementary in vitro and invivo investigations. Both of them exhibit calcium antagonist properties in the same range ofpotency as flunarizine itself. Compound 36 was also found to have significant hypolipaemicactivity in mice at 100 and 300 mg/kg po, while compound 25 proved to be clearly active in anormobar hypoxia test.
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