Benzothiazoles as effective inhibitors of cholinesterases: Kinetics and mechanism of inhibition

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216275%3A25310%2F15%3A39900202" target="_blank" >RIV/00216275:25310/15:39900202 - isvavai.cz</a>

Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

Benzothiazoles as effective inhibitors of cholinesterases: Kinetics and mechanism of inhibition

Popis výsledku v původním jazyce

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 twotypes 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.

Název v anglickém jazyce

Benzothiazoles as effective inhibitors of cholinesterases: Kinetics and mechanism of inhibition

Popis výsledku anglicky

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 twotypes 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.

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

CE - Biochemie

OECD FORD obor

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Projekt

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Návaznosti

S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2015

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Scientific Papers of the University of Pardubice, Series A, Faculty of Chemical Technology

ISSN

1211-5541

e-ISSN

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Svazek periodika

21

Číslo periodika v rámci svazku

září

Stát vydavatele periodika

CZ - Česká republika

Počet stran výsledku

13

Strana od-do

31-43

Kód UT WoS článku

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EID výsledku v databázi Scopus

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