A simple, straightforward, and highly efficient one-pot three-component synthesis of a pharmaceutically interesting kind of functionalized dihydro-6H-chromeno[4,3-b]isoxazolo[4,5-e]pyridine heterocycles has been developed based on an environmentally benign method. All synthesized compounds were evaluated for their antidiabetic activity against type 2 diabetes mellitus. The results indicated that most of the synthesized compounds exhibited moderate to good antidiabetic activity. Synthesized compound 4i demonstrated the highest inhibition of α-amylase activity (IC50 = 56.043 µg/mL). This finding suggests an approach to develop effective antidiabetic agents by incorporating pyridine core structure.
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