Synthesis and in vitro antioxidant activity of new pyrimidin/benzothiazol-substituted piperazinyl flavones.

AIM: Synthesis of novel 2(2-hydroxyphenyl) pyrimidine/benzothiazole piperazinyl-substituted flavones end evaluate their antioxidant activity. RESULTS: Six novel 2-(2-hydroxyphenyl) pyrimidine/benzothiazole-substituted flavones were synthesized, their structures were confirmed by elementary and spectral analyses. The compounds were evaluated for their in vitro antioxidant potency by employing various antioxidant assays. CONCLUSION: All tested compounds acted as scavengers of free radicals like hydroxyl (15-45%), 2,2-diphenyl-1-picrylhydrazyl• (17-48%) at 1.25 and 0.5 mM concentrations respectively. The total antioxidant status activity values of the compounds ranged from 234.1 to 464.1 µm trolox equivalent/g, the total antioxidant capacity - from 24.9 to 52.7 µm trolox equivalent per gram. Compounds incorporating the benzothiazole group on the piperazine ring were more effective antioxidants than those with the 2-(2-hydroxyphenyl) pyrimidine group.

Synthesis and antidiabetic activity of 2,4-thiazolidindione, imidazolidinedione and 2-thioxo-imidazolidine-4-one derivatives bearing 6-methyl chromonyl pharmacophore.

Numerous compounds have been prepared in order to improve the pharmacological profile of insulinotropic activities. In the present paper, we report the synthesis and the in vitro insulin releasing activity of the 6-methyl-chromonyl-2,4-thiazolidinediones (IIIa-c, IVa-c, Va-c). Compounds IIIb, IIIc, IVa-c, Va and Vc (at lower concentration; 0.001 mg/mL) were able to increase insulin release in the presence of 5.6 mmol/L glucose. In this series, the most potent compound is IVa having methyl group at N3 position of TZD ring.