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Antidiabetic Evaluation of New Pyrimidine‐Thiazoline Hybrids Endorsed With Enzyme Kinetic Studies and Computational Analysis
Testing new pyrimidine-thiazoline compounds for diabetes using enzyme activity and computer modeling
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Abstract
Compound 8j is a 3-fold more potent inhibitor of α-glucosidase compared to the standard drug acarbose.
- Molecular hybridization of pyrimidine-thiazole compounds was explored for their potential as diabetes inhibitors.
- Compound 8j showed an IC of 36.23 ± 2.41 μM against α-glucosidase and 38.42 ± 1.63 μM against α-amylase, indicating significant potency.
- Compounds 8a and 8j exhibited strong antioxidant activity, with IC values lower than those of ascorbic acid.
- Kinetic studies suggested that compounds 4b, 8g, and 8j act as noncompetitive inhibitors.
- Molecular docking studies indicated potential protein-ligand interactions for the synthesized compounds.
- ADME/T parameter analysis showed these compounds may possess better drug-like properties than acarbose.
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Key numbers
3×
α-Glucosidase Inhibition Potency Increase
IC of 36.23 ± 2.41 μM for 8j vs. 103.25 ± 1.45 μM for acarbose
2×
α-Amylase Inhibition Potency Increase
IC of 38.42 ± 1.63 μM for 8j vs. 85.00 ± 0.85 μM for acarbose
2×
DPPH Scavenging Activity Increase
IC of 37.84 μM for 8a vs. 88.40 μM for ascorbic acid