α-Amylase/α-Glucosidase-IN-11 (Compound 5d) is a isoxazolidine-isatin hybrid with significant antidiabetic activity. α-Amylase/α-Glucosidase-IN-11 competitively inhibits α-amylase ( IC 50 = 30.39 μM ) and α-glucosidase ( IC 50 = 65.1 μM ), two key digestive enzymes. α-Amylase/α-Glucosidase-IN-11 does not cross the blood-brain barrier.