New conjugates of quinoxaline - 2, 3 (1H, 4H) dione containing pioglitazone, glimepiride and thiosemicarbazide moieties were synthesized as mannich base to interpret the effect of quinoxaline on antidiabetic potential of current drugs. Quinoxalin - 2, 3 (1H, 4H) - dione was treated with respective antidiabetic moieties and thiosemicarbazide and the reaction products were purified and characterized by IR, 1H NMR, 13C NMR, Mass Spectral and elemental data. The acute oral toxicity study indicated that no mortality was observed for the synthesized compounds at a given test dose of 500 mg/Kg b.w/ p.o. Compounds were evaluated for antidiabetic activity in male Wistar albino rats. Thiosemicarbazide of quinoxaline mannich base showed significant antidiabetic activity with p value of < 0.001 and comparable with Pioglitazone. Pioglitazone derivatives exhibited better onset of action than parent pioglitazone and also recorded the potent hypoglycemic profile than parent drug. Docking analysis was performed to support the binding affinity of new Ligands on PPAR2 receptor.
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