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

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. This article is protected by copyright. All rights reserved.