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Benzothiazoles as effective inhibitors of cholinesterases: Kinetics and mechanism of inhibition
Year: 2015
Type of publication: článek v odborném periodiku
Name of source: Scientific Papers of the University of Pardubice, Series A, Faculty of Chemical Technology
Page from-to: 31-43
Titles:
Language Name Abstract Keywords
cze Benzothiazoly jako účinné inhibitory cholinesteráz: Kinetika a mechanismus inhibice Cílem naši studie bylo stanovení inhibiční účinnosti testovaných benzothiazolů, které patří do skupiny inhibitorů cholinesteráz. Byla sledovaná kinetika hydrolýzy acetylcholinu a acetylthiocholinu reakce neinhibované a inhibované za použití dvou enzymů, acetylcholinesterázy a butyrylcholinesterázy. Byly použité dvě metody, Ellmanová a pH-statová metoda. benzothiazoly, cholinesterázy, inhibice, kinetické parametry
eng Benzothiazoles as effective inhibitors of cholinesterases: Kinetics and mechanism of inhibition The aim of our study was to determine the inhibition efficiency of the benzothiazoles tested, representing potential inhibitors of cholinesterases. (Reaction) kinetics of hydrolyses of acetylcholine and acetylthiocholine, uninhibited and inhibited by two types of enzyme, acetylcholinesterase, and butyrylcholinesterase, has been studied. Two methods for the determination of enzymatic hydrolysis were used, Ellman’s and pH-stat method and, totally, twelve inhibitors (benzothiazoles) selected to study the inhibited hydrolysis. The kinetic parameters of uninhibited and inhibited hydrolyses have been determined and, based on our current results of inhibition rate constant, 2,2,3,3-tetrafluoropropyl (S)-1-(R)-1-(6-fluorobenzo[d]thiazole)ethyl-carbamoyl-2-methylpropylcarbamate found to be the best inhibitor of cholinesterases from the palette of the inhibiting substances tested. benzothiazoles, cholinesterases, inhibition, kinetics parameters

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