In order to produce potent new leads for antidiabetic drugs, a new series of isoindoline-1,3-dione analogues bearing aryl sulfonylurea moieties were synthesized and screened for their antihyperglycemic activity. Some of newly synthesized compounds were identified as active antihyperglycemic agents. Compounds N-(cyclohexylcarbamoyl)-4-[2-(1,3-dioxoisoindolin-2-yl) ethyl]benzenesulfon-amide(VII_o),N-(cyclopentylcabamoyl)-4-[2-(1,3-dioxoiso- indolin-2-yl)ethyl] benzene sulfonamide (VII_p), N-(butylcabamoyl)-4-[2-(1,3-dioxoisoindolin-2-yl)ethyl]benzenesulfonamide(VII_q),N-(cyclohexylcarbamoyl) -4- [ ( 1, 3- dioxo - isoindolin- 2 – yl ) methyl ] benzenesulfonamide (VII_h)  and N-(propylcabamoyl)-4-[2-(1,3-dioxoisoindolin-2-yl)ethyl]benzenesulfonamide (VII_r)  proved to be the most active members of this study, as compered to  to the reference gliclazide. They showed serum glucose reduction values of 52%, 48% 45%, 44% and 44%,  respectively. The detailed  synthesis and biological screening data are reported.