The new TZD derivatives prepared (i.e. A1, A2, A5, B2, C1 and D1) were screened in vivo for acute oral toxicity study for the doses of 30 and 100 mg/kg in Wistar rats and were found to be safe as they did not show any treatment related adverse effects. So these six derivatives were evaluated for antidiabetic activity using the experimental model of diabetes induced by alloxan in rats for acute as well as subacute study.The results of the study revealed that most of the compounds tested showed moderate to good antidiabetic activity. The compound C1 was found to be the most active in all synthesized compounds which have nearly similar glucose lowering activity as that of standard drugs i.e. metformin and pioglitazone at dose of 100 mg/kg of body weight.