Synthesis of new thiazol-4-one derivatives and investigation of their biological activities
2025
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Advisor: Prof. Dr. Nalan Gündoğdu Karaburun
Abstract (EN)
It is thought that Alzheimer's disease (AD), which is a neurodegenerative disease that is progressive and age-related and brings serious care cost obligations to countries, may become more common than cancer in the future due to the increase in its population. Studies conducted for the treatment of this disease have not achieved their goal in the context of rational treatment due to uncertainties in its etiology. In this master's thesis, a series of new thiazol-4-one derivative compounds were designed and synthesized based on thiazole, morpholine, hydrazone and chalcone structures found in the structures of donepezil and target compounds obtained as a result of literature review and shown to have AChE, BChE, MAO-A or MAO-B inhibitory activities and their structures were identified by IR, 1H-NMR, 13C-NMR methods. According to the biological activity results performed and evaluated with reference compounds, the most potent inhibitory activity was shown by the '4-methoxy benzylidene' derivative compound 4c for AChE, BChE and MAO-B enzymes, and the '4-dimethylamine benzylidene' derivative compound 4e, which exhibits the closest profile and is the most effective compound against MAO-A. These compounds, which were subjected to molecular docking and molecular dynamics analysis for the AChE enzyme and whose interactions with the active sites of the enzyme were examined, showed results that could play a role in the treatment of AD.
Author
Dr. Burak Yavuz
Institution
How to Cite
Burak Yavuz (Master Thesis). Synthesis of new thiazol-4-one derivatives and investigation of their biological activities, 2025, Anadolu University.
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