Premium
Synthesis and biological evaluation of 2‐acylbenzofuranes as novel α‐glucosidase inhibitors with hypoglycemic activity
Author(s) -
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.
Publication year - 2017
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13038
Subject(s) - acarbose , benzofuran , chemistry , potency , docking (animal) , pharmacology , structure–activity relationship , enzyme , stereochemistry , biochemistry , in vitro , medicine , nursing
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 IC 50 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.