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Int J Biol Macromol ; 190: 301-318, 2021 Nov 01.
Article in English | MEDLINE | ID: mdl-34481854

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.


Subject(s)
Computer Simulation , Glycoside Hydrolase Inhibitors/pharmacology , Hypoglycemic Agents/pharmacology , Indoles/chemical synthesis , Indoles/pharmacology , alpha-Amylases/antagonists & inhibitors , alpha-Glucosidases/metabolism , Catalytic Domain , Glycoside Hydrolase Inhibitors/chemistry , Hydrogen Bonding , Hypoglycemic Agents/chemistry , Indoles/chemistry , Kinetics , Molecular Docking Simulation , Saccharomyces cerevisiae/enzymology , Structure-Activity Relationship
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