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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 [Int J Biol Macromol] 2021 Nov 01; Vol. 190, pp. 301-318. Date of Electronic Publication: 2021 Sep 02. - Publication Year :
- 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 (IC <subscript>50</subscript>  = 3.80 to 47.50 μM), and α-glucosidase inhibitory interactions (IC <subscript>50</subscript>  = 3.10-52.20 μM) in comparison with standard acarbose (IC <subscript>50</subscript>  = 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.<br /> (Copyright © 2021 Elsevier B.V. All rights reserved.)
- Subjects :
- Catalytic Domain
Glycoside Hydrolase Inhibitors chemistry
Hydrogen Bonding
Hypoglycemic Agents chemistry
Indoles chemistry
Kinetics
Molecular Docking Simulation
Saccharomyces cerevisiae enzymology
Structure-Activity Relationship
Computer Simulation
Glycoside Hydrolase Inhibitors pharmacology
Hypoglycemic Agents pharmacology
Indoles chemical synthesis
Indoles pharmacology
alpha-Amylases antagonists & inhibitors
alpha-Glucosidases metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1879-0003
- Volume :
- 190
- Database :
- MEDLINE
- Journal :
- International journal of biological macromolecules
- Publication Type :
- Academic Journal
- Accession number :
- 34481854
- Full Text :
- https://doi.org/10.1016/j.ijbiomac.2021.08.207