Synthesis, Characterization and Bioactivity Study of Potential Acetylcholinesterase Inhibitor Pyridinium Derivatives
Project no. 29557 · Status: Kapanmış · 2023
Summary
<p>Alzheimer's disease is one of the most common forms of dementia. It is a progressive, irreversible, neurodegenerative disease characterized by memory loss. Alzheimer's is a chronic syndrome of the central nervous system, which causes a decrease in cognitive function and language ability, and decreases in the memory capacity of the patients over time. A treatment system that will completely cure the disease has not yet been found. There are studies that slow the progression of the disease. These studies still continue today.</p><p> Cholinergic deficiency is associated with Alzheimer's and one of the most effective treatment modalities is to increase cholinergic conduction. Various cholinesterase inhibitors have been developed for the treatment of Alzheimer's, including naturally derived inhibitors, synthetic analogs, and hybrids. Currently, the drugs available for Alzheimer's are predominantly cholinesterase inhibitors. However, the effectiveness of these drugs is limited as they can cause adverse side effects and cannot completely stop the progression of the disease. Since Alzheimer's disease is a multifactorial disease, dual and multitargeted inhibitors have been developed. Acetylcholinesterase inhibitors offer hope in the definitive treatment of the disease.</p><p>In our thesis, we aimed to synthesize a new pyridinium derivative as a result of the quaternization of 2,6-dichlorobenzyl chloride with the intermediate product obtained by the Claisen-Schmidt condensation reaction of 4-chloroacetophenone with pyridine-3-carbaldehyde. Then, the final compound was purified and its chemical structure was analysed with spectroscopic methods (IR, 1H NMR). The inhibitory activity on AChE enyzme was determined according to the modified Ellman method.</p><p> </p>