Abstract
Neurodegenerative diseases in which the decrease of the acetylcholine is observed are growing worldwide. In the present study, a series of new arylaminopropanone derivatives with N-phenylcarbamate moiety (1–16) were prepared as potential acetylcholinesterase and butyrylcholinesterase inhibitors. In vitro enzyme assays were performed; the results are expressed as a percentage of inhibition and the IC50 values. The inhibitory activities were compared with reference drugs galantamine and rivastigmine showing piperidine derivatives (1–3) as the most potent. A possible mechanism of action for these compounds was determined from a molecular modelling study by using combined techniques of docking, molecular dynamics simulations and quantum mechanics calculations.
Highlights
Dementia is a syndrome caused by a variety of brain illnesses, whose worldwide incidence and prevalence is still growing
According to the cholinergic hypothesis, a loss of cholinergic activity is commonly observed in the brains of Alzheimer’s disease (AD) patients and experimental data confirmed the role of acetylcholine (ACh) in learning and memory [2,3]
The present study describes the synthesis of novel carbamate derivatives with arylaminopropanone structure designed as potential cholinesterase inhibitors
Summary
Dementia is a syndrome caused by a variety of brain illnesses, whose worldwide incidence and prevalence is still growing. Alzheimer’s disease (AD) is the most common form of dementia. It includes more than 65 % diagnostic cases representing 5.4 million new patients every year. This neurodegenerative disease is characterized by the disturbance of multiple higher cortical functions like memory, orientation, comprehension, and other cognitive functions [1]. AD is progressive, leading to an irreversible loss of neurons. According to the cholinergic hypothesis, a loss of cholinergic activity is commonly observed in the brains of AD patients and experimental data confirmed the role of acetylcholine (ACh) in learning and memory [2,3]
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