1. Synthesis and biological evaluation of 2-acylbenzofuranes as novel α-glucosidase inhibitors with hypoglycemic activity
- Author
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Alexander A. Spasov, Tatyana Yu Prokhorova, Diana R. Muleeva, Denis A. Babkov, Yuri N. Klimochkin, Vitaly A. Osyanin, Dmitry V. Osipov, Ekaterina A. Sturova, and Maxim R. Demidov
- Subjects
Male ,Saccharomyces cerevisiae ,010402 general chemistry ,01 natural sciences ,Biochemistry ,Streptozocin ,Diabetes Mellitus, Experimental ,chemistry.chemical_compound ,Drug Discovery ,medicine ,Animals ,Hypoglycemic Agents ,Potency ,Glycoside Hydrolase Inhibitors ,Rats, Wistar ,Benzofuran ,Benzofurans ,Biological evaluation ,Acarbose ,Pharmacology ,chemistry.chemical_classification ,Binding Sites ,010405 organic chemistry ,α glucosidase ,Organic Chemistry ,alpha-Glucosidases ,Glucose Tolerance Test ,Reference drug ,Protein Structure, Tertiary ,Rats ,0104 chemical sciences ,Molecular Docking Simulation ,Enzyme ,chemistry ,Docking (molecular) ,Molecular Medicine ,medicine.drug - 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 to structure-activity relationships to direct further development of these novel hypoglycemic agents. This article is protected by copyright. All rights reserved.
- Published
- 2017