Yeni Tiyazol türevleri ve biyolojik etkilerinin araştırılması
2023
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Advisor: Prof. Dr. Leyla Yurttaş
Abstract (EN)
In this thesis, it was aimed to design and synthesize a total of 12 compounds (5a-5l) containing the thiazole ring, which is a potential structure that can be used in the treatment of neurodegenerative disorders such as Alzheimer's and Parkinson's diseases. N-[4-(4-Acetamidophenyl)thiazol-2-yl)-]2-((heteroaryl)thio)propanamide (5a-5l) derivative compounds were analyzed using various techniques such as IR, NMR, and HRMS, and their physical properties were determined. The synthesized compounds were then tested for their potential inhibitory activity on acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and monoamine oxidase (MAO-A and MAO-B) enzymes. The compounds showed remarkable activity as AChE inhibitors, of which compounds 5d, 5e and 5j exhibited the highest AChE inhibitory activity. However, the inhibitory activities of the compounds against both the BChE and the MAOs were weak. The three most effective compounds, the way they bind to protein sites, the bonds they make, and the effects of time-environmental variables on these interactions were investigated by molecular docking and dynamic simulation docking analyses. This study highlights that thiazole compounds are a good framework for the treatment of neurodegenerative disorders in drug development studies.
Author
Dr. Abd Al Rahman Asfour
How to Cite
Abd Al Rahman Asfour (Master Thesis). Yeni Tiyazol türevleri ve biyolojik etkilerinin araştırılması, 2023, Anadolu University.
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