Identifies oxazin‐4‐one derivatives as potent inhibitors of key enzymes in diabetes and Alzheimer's disease, suggesting new therapeutic avenues.
Oxazin‐4‐one‐based synthetic derivatives ( 1–30 ) were evaluated for inhibitory activity against α ‐amylase, α ‐glucosidase, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). The molecules demonstrated potent inhibition, with IC 50 values of 18.65 ± 0.23 µ M to 37.70 ± 0.06 µ M for α ‐amylase and 15.68 ± 0.36 to 37.47 ± 0.13 µ M for α ‐glucosidase, comparable to the reference drug acarbose (IC 50 = 16.98 ± 0.12 µ M and 14.19 ± 0.06 µ M, respectively). Antioxidant capacity was quantified using DPPH and ABTS radical scavenging assays. Kinetic analysis identified competitive and mixed‐type inhibition mechanisms, while molecular docking simulations characterized the binding interactions within the active sites. Overall, these findings suggest that oxazin‐4‐one derivatives may serve as promising multitarget starting points for further optimization toward metabolic, neurodegenerative, and oxidative‐stress‐related pathways.
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Khan et al. (2026) studied this question.
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