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:
benzofurans; diabetes; α-glucosidase.
© 2017 John Wiley & Sons A/S.
MeSH terms
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Animals
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Benzofurans / chemistry*
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Benzofurans / metabolism
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Benzofurans / therapeutic use
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Binding Sites
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Diabetes Mellitus, Experimental / chemically induced
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Diabetes Mellitus, Experimental / drug therapy
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Glucose Tolerance Test
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Glycoside Hydrolase Inhibitors / chemical synthesis*
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Glycoside Hydrolase Inhibitors / metabolism
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Glycoside Hydrolase Inhibitors / therapeutic use
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Hypoglycemic Agents / chemical synthesis*
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Hypoglycemic Agents / metabolism
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Hypoglycemic Agents / therapeutic use
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Male
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Molecular Docking Simulation
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Protein Structure, Tertiary
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Rats
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Rats, Wistar
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Saccharomyces cerevisiae / enzymology
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Streptozocin / toxicity
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alpha-Glucosidases / chemistry*
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alpha-Glucosidases / metabolism
Substances
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Benzofurans
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Glycoside Hydrolase Inhibitors
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Hypoglycemic Agents
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Streptozocin
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alpha-Glucosidases