Design, synthesis and biological activity studies of new compounds to be used in alzheimer's disease treatment
2019
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Advisor: Prof. Dr. Yusuf Özkay
Abstract (EN)
Alzheimer's disease (AD) is a progressive and neurodegenerative disease primarily seen in the elderly population, clinically characterized by memory and cognitive impairment. The importance of disease increase because of some reasons; the etiology of the disease has not been determined yet, increase in patient population over the years, absence of radical treatment, high cost of treatment and care, significant reduction in quality of life of patients, and these lead to direct researchers to this field. In this PhD thesis, 42 new indan-1-on derivatives were designed and synthesized based on the chemical structure of donepezil molecule, which is the most preferred and most favorable treatment response in the treatment of AD. The structures of the compounds were determined by IR, 1H and 13C NMR and mass spectroscopic methods. Inhibition studies on the cholinesterase (ChE) enzymes, monoamine oxidase A and B (MAO) enzymes, beta amyloid plaque inhibition test, antioxidant activity and cytotoxicity effect studies of the compounds were performed. In the compound series, two groups of compounds are noted due to their strong enzyme inhibition profiles and their strong binding modes with the enzyme active sites. Compounds D28-D30 and D37-D39 show potent inhibitory activity on AChE, BChE and MAO-B enzymes, inhibition of beta amyloid plaque aggregation and high antioxidant activity. Owing to their multiple effects, it is thought that the related compounds may play a role in the both symptomatic and palliative treatment of AD.
Author
Dr. Begüm Nurpelin Sağlık
How to Cite
Begüm Nurpelin Sağlık (Doctorate thesis). Design, synthesis and biological activity studies of new compounds to be used in alzheimer's disease treatment, 2019, Anadolu University.
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