Synthesis and biological evaluation of 2-acylbenzofuranes as novel α-glucosidase inhibitors with hypoglycemic activity
| Autor: | Alexander A. Spasov, Tatyana Yu Prokhorova, Diana R. Muleeva, Denis A. Babkov, Yuri N. Klimochkin, Vitaly A. Osyanin, Dmitry V. Osipov, Ekaterina A. Sturova, Maxim R. Demidov |
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| Rok vydání: | 2017 |
| Předmět: |
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 |
| Zdroj: | Chemical Biology & Drug Design. 90:1184-1189 |
| ISSN: | 1747-0277 |
| DOI: | 10.1111/cbdd.13038 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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