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Fluorinated indeno-quinoxaline bearing thiazole moieties as hypoglycaemic agents targeting α -amylase, and α -glucosidase: synthesis, molecular docking, and ADMET studies
Fluorinated compounds with thiazole parts as blood sugar-lowering agents targeting digestive enzymes: creation, computer modeling, and safety studies
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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.
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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