1. Synthesis and biological evaluation of 2-acylbenzofuranes as novel α-glucosidase inhibitors with hypoglycemic activity.
- Author
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Spasov AA, Babkov DA, Prokhorova TY, Sturova EA, Muleeva DR, Demidov MR, Osipov DV, Osyanin VA, and Klimochkin YN
- Subjects
- Animals, Benzofurans metabolism, Benzofurans therapeutic use, Binding Sites, Diabetes Mellitus, Experimental chemically induced, Diabetes Mellitus, Experimental drug therapy, Glucose Tolerance Test, Glycoside Hydrolase Inhibitors metabolism, Glycoside Hydrolase Inhibitors therapeutic use, Hypoglycemic Agents metabolism, Hypoglycemic Agents therapeutic use, Male, Molecular Docking Simulation, Protein Structure, Tertiary, Rats, Rats, Wistar, Saccharomyces cerevisiae enzymology, Streptozocin toxicity, alpha-Glucosidases metabolism, Benzofurans chemistry, Glycoside Hydrolase Inhibitors chemical synthesis, Hypoglycemic Agents chemical synthesis, alpha-Glucosidases chemistry
- 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 IC
50 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., (© 2017 John Wiley & Sons A/S.)- Published
- 2017
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