Design, synthesis and biological activity studies of new cholinesterase and monoamine oxidase enzyme inhibitors

Alzheimer's disease, which is considered the most common cause of dementia, is a progressive and degenerative disease that affects cognitive functions. Currently used treatments are symptomatic treatments aimed at increasing reduced cholinergic activity. Due to the predicted increases in the number of patients, the increase in the cost of treatment and the long duration of the treatment process, there is a great need for the development of new drugs in the treatment of Alzheimer's disease worldwide. Parkinson's disease is a chronic and progressive disease that causes slowing of movements and involuntary movement disorders due to the loss of dopaminergic neurons in the brain. Since the pathophysiological mechanisms causing the disease have not been fully elucidated, the current treatments consist of symptomatic treatments aimed at improving the quality of life of patients. Due to the fact that it can be seen in different social and economic conditions, drug development studies in this field have gained importance all over the world. In this PhD thesis, benzazole derivatives containing chalcone structure were synthesized and their structure was elucidated by 1H NMR, 13C NMR and mass spectroscopy. The inhibitory activities of the compounds on the ChE and MAO enzymes have been tested. The compounds in the series do not show significant activity on BChE, MAO-A and MAO-B enzymes; however, it was determined that all compounds exhibited high activity against the AChE enzyme. It was determined that 3f and 3l coded compounds among the synthesized compounds showed strong inhibitory activity on AChE enzyme. Molecular modeling studies were performed for the most active compounds, 3f and 3l, and their interactions with the corresponding enzyme were determined. Keywords: Benzazole, Cholinesterase, Monoamine oxidase, Chalcone