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  • Title: Synthesis and biological evaluation of 2-acylbenzofuranes as novel α-glucosidase inhibitors with hypoglycemic activity.
    Author: Spasov AA, Babkov DA, Prokhorova TY, Sturova EA, Muleeva DR, Demidov MR, Osipov DV, Osyanin VA, Klimochkin YN.
    Journal: Chem Biol Drug Des; 2017 Dec; 90(6):1184-1189. PubMed ID: 28585419.
    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 into structure-activity relationships to direct further development of these novel hypoglycemic agents.
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