Diabetes is one of the major health problems, the world is facing today. It is rising in an alarming rate necessitating alternative treatment methods. The present study has been undertaken to evaluate the anti-diabetic activity of marmelosin extracted from Aegle marmelos. The extraction of plant material in different solvent like petroleum ether, chloroform and ethanol by soxhelation was carried out. Marmelosin was separated out from extraction of Aegle marmelos by Column chromatography methods. Marmelosin derivatives were synthesized using Nitration, Sulphonation and Bromination reaction. The synthesized compounds were evaluated for anti-diabetic activitiy. The effect of marmelosin and its derivatives on hyperglycemia induced with alloxan on repeated administration was studied on male wistar rat. The estimation of blood sugar was carried out by the method GOD-PAP enzymatic method. The results were satisfactory, as significant decrease in the blood glucose levels after repeated administration was observed.