Design, Synthesis, And Biological Evaluation Of Some 1,2,4-Triazin-Linked Oxazole Derivatives To Treat Alzheimer's Disease
DOI:
https://doi.org/10.64252/1hps8c12Keywords:
Acetylcholine, AChE inhibitors, Chemistry, and Alzheimer's diseaseAbstract
Alzheimer’s disease (AD) is a complex neurodegenerative disorder characterized by progressive cognitive decline, memory impairment, and synaptic dysfunction. A significant pathological hallmark of AD is the deficiency of cholinergic neurotransmission, primarily caused by excessive activity of acetylcholinesterase (AChE), which degrades acetylcholine in the synaptic cleft.
The compounds were synthesized via a multistep reaction pathway involving the formation of diphenyl-1,2,4-triazine cores followed by condensation with appropriately substituted oxazole moieties. The structural identity of the synthesized compounds was confirmed using spectroscopic techniques, including IR, NMR, and mass spectrometry. All synthesized derivatives were subjected to in vitro AChE inhibition assay using Ellman's method. The results revealed that several compounds demonstrated strong inhibitory activity, with IC₅₀ values in the low micromolar range.
In conclusion, the diphenyl-1,2,4-triazin-linked oxazole derivatives presented in this study represent a promising new class of AChE inhibitors for the treatment of AD. Their superior efficacy over oxazole analogs makes them attractive candidates for further development.
