Synthesis of Novel Thiazolyl-Hydrazine Derivatives and Activity Studies of Acetylcholinesterase (AChE) and Butyrylcholinesterase (BuChE)

Abstract

Alzheimer's disease (AD) has been associated with ecreased cognitive function, memory loss, and dementia due to the death of brain cells over time. Existence of limiting practices in the treatment of AD, and the fact that the disease ranks third in health expenditures in the world after cancer and heart diseases, directs researchers to early diagnosis and new treatment methods on AD. Today, it is thought that there is a direct relationship between cholinergic abnormalities and AD. Studies have shown that acetylcholine (ACh) level increases due to acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibition can improve cognitive impairment in the initial stages of Alzheimer's disease. The best method to increase these ACh levels is to suppress the AChE or BuChE enzymes that break down ACh. Therefore, in this study, substituted thiazolylhydrazine derivatives were designed, synthesized and their cholinesterase inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzymes against AD were investigated. The structures of the target compounds were illuminated by 1H NMR/13C NMR analysis methods. The effects of the target compounds on the on AChE and BuChE enzymes were evaluated using the Ellman process and as a result of the enzyme inhibiton studies of the target compounds, it was determined that the 3d compound showed moderate butyrylcholinesterase activity.