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- Title
Synthesis and biological evaluation of 2-acylbenzofuranes as novel α-glucosidase inhibitors with hypoglycemic activity.
- Authors
Spasov, Alexander A.; Babkov, Denis A.; Prokhorova, Tatyana Yu; Sturova, Ekaterina A.; Muleeva, Diana R.; Demidov, Maxim R.; Osipov, Dmitry V.; Osyanin, Vitaly A.; Klimochkin, Yuri N.
- 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 μ m, 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.
- Subjects
BENZOFURAN; HETEROCYCLIC compound derivatives; BENZOFURAN synthesis; GLUCOSIDASE synthesis; GLUCOSIDASE inhibitors; HYPOGLYCEMIC agents
- Publication
Chemical Biology & Drug Design, 2017, Vol 90, Issue 6, p1184
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.13038