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Synthesis and biological evaluation of 2-acylbenzofuranes as novel α-glucosidase inhibitors with hypoglycemic activity
- Source :
- Chemical Biology & Drug Design. 90:1184-1189
- Publication Year :
- 2017
- Publisher :
- Wiley, 2017.
-
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.
- 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
Subjects
Details
- ISSN :
- 17470277
- Volume :
- 90
- Database :
- OpenAIRE
- Journal :
- Chemical Biology & Drug Design
- Accession number :
- edsair.doi.dedup.....5f4e4d1f559c62463f9a16253e62260c