Synthesis and biological evaluation of 2‐acylbenzofuranes as novel α‐glucosidase inhibitors with hypoglycemic activity
- 3 July 2017
- journal article
- Published by Wiley in Chemical Biology & Drug Design
- Vol. 90 (6), 1184-1189
- https://doi.org/10.1111/cbdd.13038
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.Keywords
Funding Information
- Russian Science Foundation (14-25-00139)
- Russian Foundation for Basic Research (15-43-02304 r_povolzhye_a)
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