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

Result code in 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>

Result on the web

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DOI - Digital Object Identifier

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Result language

angličtina

Original language name

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

Original language description

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.

Czech name

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Czech description

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Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

CE - Biochemistry

OECD FORD branch

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Project

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Continuities

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

Publication year

2015

Confidentiality

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

Name of the periodical

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

ISSN

1211-5541

e-ISSN

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Volume of the periodical

21

Issue of the periodical within the volume

září

Country of publishing house

CZ - CZECH REPUBLIC

Number of pages

13

Pages from-to

31-43

UT code for WoS article

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EID of the result in the Scopus database

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