Synthesis and biological evaluation of 2-acylbenzofuranes as novel α-glucosidase inhibitors with hypoglycemic activity

Abstract

A series of benzofuran derivatives was synthesized as analogues of known natural α-glucosidase inhibitors. Their activity was evaluated in enzymatic assay and in rat model of diabetes mellitus. Newly identified inhibitors demonstrate significant potency with IC₅₀ values ranging from 6.50 to 722.2 μM, as well as hypoglycemic activity exceeding the reference drug acarbose. Docking simulations provided insight to structure-activity relationships to direct further development of these novel hypoglycemic agents.

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A novel series of benzofuran derivatives was synthesized and evaluated as potential antidiabetic agents. Synthesized compounds show higher inhibitory activity against α-glucosidase than acarbose. Lead compounds effectively prevent postprandial hyperglycemia in diabetic rats encouraging further structure optimizations.

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