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Synthesis and characterization of new N-phenylcarbamates as potential inhibitors of cholinesterases

Authors: Horáková Eva | Vorčáková Katarína | Drabina Pavel | Sedlák Miloš

Year: 2018

Type of publication: ostatní - přednáška nebo poster

Page from-to: nestránkováno

Titles:

Language	Name	Abstract	Keywords
eng	Synthesis and characterization of new N-phenylcarbamates as potential inhibitors of cholinesterases	Alzheimerʼs disease (AD) is known as progressive neurodegenerative brain disorder, whose exact cause of attendance is still unknown.1 One of clinical manifestation of AD is connected with low acetylcholine (ACh) concentration in cholinergic synapses.2 Currently, symptomatic treatment of AD is based on inhibition of acetylcholinesterases (AChE) and butyrylcholinesterases (BChE) by wide-range group of inhibitors of both ChEs, e.g. carbamates. Generally, carbamate inhibitors, such as AD’s drug Rivastigmine, act as pseudo-reversible inhibitors of ChEs.3 The aim of this work was preparation and characterization of two series of new carbamate derivatives: i) N-phenylcarbamates with additional carbamate group (1-12) and ii) N-phenylcarbamates with monosaccharide moiety (13-24). All of these carbamates were tested as potential inhibibitors of ChEs and the inhibitory activity was compared with drugs Galanthamine and Rivastigmine. Furthermore partition coefficients Pow, type of inhibition and molecular docking of chosen compound was studied.4	N-Phenylcarbamates; inhibibitors; cholinesterases