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Background: Thiazolidinediones (TZDs) and sulfonamides are important and highly consumption class of antidiabetic drugs having insulin sensitizing and stimulating properties in patients with type 2 diabetes, respectively. Objective: In this paper, some novel benzothiazole derivatives of TZD-sulfonamides were synthesized (I-IV) and evaluated for anti-hyperglycemic and anti-hyperlipidemic activities in the STZ-induced diabetic rat model. Results: Results indicated that all new conjugated compounds showed significant hypoglycemic activities compared to control animals that were better for I and IV than others. Moreover, these new compounds displayed high efficiency for lowering lipid profiles as compared to control and standard (Pioglitazone) groups that was significant and higher for I than others. Conclusion: It is concluded that these new conjugated TZD-sulfonamide-benzothiazoles (I-IV) can indicate useful results for hypoglycemic and hypolipidemic activities compared to control and standard groups, respectively with different mechanism that is closer to TZDs' analogs.