Synthesis of New Thiocarbamates and Evaluation of their Cholinesterase Inhibitory Effect.

VAYEGHAN, BAHAREH DINDARI

Alzheimer's disease is a neurodegenerative disorder in which cholinergic neurons destroy specific parts of the brain and decrease acetylcholine levels. Therefore, enhancing cholinergic function, which increases acetylcholine levels in the brain, has been proposed as a perspective for symptomatic treatment of Alzheimer's disease. For this reason, cholinesterase inhibitors are one of the most commonly used drugs for Alzheimer's patients today. In this study, we are investigating the availability of novel compounds of cholinesterase inhibitors. After reviewing the results of previous studies, a number of compounds were suggested and synthesized as acetylcholinesterase inhibitors. Two final products called 3- (2 and 6-dichlorophenyl) -3-oxo-1-phenylpropyl 2-chlorobenzene carbamodiodioate and1- (4- chlorophyll) -3-phenylpropyl hydroxylcarbamodiodioate were synthesized as Cholinesterase inhibitors. To synthesize each of these two products, two intermediates were first provided and these inhibitors were prepared from their reaction. In the next step, by using docking studies and computational methods, the intensity and type of interaction of the designed molecules and the enzyme were estimated and finally synthesized for these compounds, with the addition of the intermediate compound 1 The structure of intermediate compound 2 and the final compound were confirmed by spectroscopy. The new compound is obtained. Then, a quantitative study was performed on the structure-activity relationship of a batch of compounds and a model was presented to estimate their cholinesterase activity.

ALZHEIMER'S disease; ACETYLCHOLINESTERASE inhibitors; ACETYLCHOLINESTERASE; MOLECULAR docking; CHOLINESTERASE inhibitors; PARASYMPATHOMIMETIC agents

International Journal of Pharmaceutical Research (09752366), 2020, Vol 12, Issue 1, p49

0975-2366

Academic Journal

10.31838/ijpr/2020.12.01.027