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Synthesis of indole derivatives as diabetics II inhibitors and enzymatic kinetics study of α-glucosidase and α-amylase along with their in-silico study
- Source :
- International Journal of Biological Macromolecules. 190:301-318
- Publication Year :
- 2021
- Publisher :
- Elsevier BV, 2021.
-
Abstract
- In this study, we have investigated a series of indole-based compounds for their inhibitory study against pancreatic α-amylase and intestinal α-glucosidase activity. Inhibitors of carbohydrate degrading enzymes appear to have an essential role as antidiabetic drugs. All analogous exhibited good to moderate α-amylase (IC50 = 3.80 to 47.50 μM), and α-glucosidase inhibitory interactions (IC50 = 3.10–52.20 μM) in comparison with standard acarbose (IC50 = 12.28 μM and 11.29 μM). The analogues 4, 11, 12, 15, 14 and 17 had good activity potential both for enzymes inhibitory interactions. Structure activity relationships were deliberated to propose the influence of substituents on the inhibitory potential of analogues. Docking studies revealed the interaction of more potential analogues and enzyme active site. Further, we studied their kinetic study of most active compounds showed that compounds 15, 14, 12, 17 and 11 are competitive for α-amylase and non- competitive for α-glucosidase.
- Subjects :
- Indoles
Saccharomyces cerevisiae
Inhibitory postsynaptic potential
Biochemistry
Structure-Activity Relationship
Structural Biology
Catalytic Domain
medicine
Hypoglycemic Agents
Computer Simulation
Glycoside Hydrolase Inhibitors
Amylase
Molecular Biology
Acarbose
Indole test
chemistry.chemical_classification
biology
Chemistry
Active site
Hydrogen Bonding
alpha-Glucosidases
General Medicine
Carbohydrate
Molecular Docking Simulation
Kinetics
Enzyme
Docking (molecular)
biology.protein
alpha-Amylases
medicine.drug
Subjects
Details
- ISSN :
- 01418130
- Volume :
- 190
- Database :
- OpenAIRE
- Journal :
- International Journal of Biological Macromolecules
- Accession number :
- edsair.doi.dedup.....8834be7ecdb0ce57d9e6a34e2e103adf