Fluorinated indeno-quinoxaline bearing thiazole moieties as hypoglycaemic agents targeting α -amylase, and α -glucosidase: synthesis, molecular docking, and ADMET studies

Jun 24, 2024Journal of enzyme inhibition and medicinal chemistry

Fluorinated compounds with thiazole parts as blood sugar-lowering agents targeting digestive enzymes: creation, computer modeling, and safety studies

AI simplified

Abstract

Four thiazole hybrids showed moderate to potent activity against α-glucosidase and α-amylase enzymes, with IC values ranging from 0.982 ± 0.04 to 10.19 ± 0.21 μM for α-glucosidase inhibition.

  • Inhibition of α-glucosidase and α-amylase may help in managing blood glucose levels for diabetes treatment.
  • The thiazole hybrids were tested on STZ-induced diabetic mice for their hypoglycaemic effects.
  • All synthesized compounds were evaluated for their effects on plasma insulin, urea, creatinine, GSH, MDA, ALT, AST, and total cholesterol.
  • The most potent compounds exhibited IC values for α-glucosidase inhibition significantly higher than that of the standard medication acarbose.
  • In vitro and in silico studies were conducted to analyze the interactions of these hybrids with the target enzymes.

AI simplified

Key numbers

0.982 ± 0.04 μM
α-Glucosidase Inhibition IC
IC value for the most potent compound against α-glucosidase
17.58 ± 0.74 μM
α-Amylase Inhibition IC
IC value for the compound against α-amylase
Significant decrease
Blood Glucose Reduction
Observed effect in STZ-induced diabetic mice

Full Text

We can’t show the full text here under this license. Use the link below to read it at the source.

what lands in your inbox each week:

  • 📚7 fresh studies
  • 📝plain-language summaries
  • direct links to original studies
  • 🏅top journal indicators
  • 📅weekly delivery
  • 🧘‍♂️always free