Back to Search Start Over

Synthesis of indole derivatives as diabetics II inhibitors and enzymatic kinetics study of α-glucosidase and α-amylase along with their in-silico study

Authors :
Sridevi Chigurupati
Muhammad Nawaz
Fazal Rahim
Vijayan Venugopal
Noor B. Almandil
Faisal Nawaz
Nizam Uddin
Suprava Das
Abdul Wadood
Ahlam Sayer Alrashedy
Naveed Iqbal
Khalid Mohammed Khan
Muhammad Taha
El Hassane Anouar
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.

Details

ISSN :
01418130
Volume :
190
Database :
OpenAIRE
Journal :
International Journal of Biological Macromolecules
Accession number :
edsair.doi.dedup.....8834be7ecdb0ce57d9e6a34e2e103adf