Synthesis and in vitro evaluation of novel N-cycloalkylcarbamates as potential cholinesterase inhibitors

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216275%3A25310%2F17%3A39910687" target="_blank" >RIV/00216275:25310/17:39910687 - isvavai.cz</a>

Result on the web

<a href="http://dx.doi.org/10.1007/s00706-017-2026-5" target="_blank" >http://dx.doi.org/10.1007/s00706-017-2026-5</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1007/s00706-017-2026-5" target="_blank" >10.1007/s00706-017-2026-5</a>

Result language

angličtina

Original language name

Synthesis and in vitro evaluation of novel N-cycloalkylcarbamates as potential cholinesterase inhibitors

Original language description

This present paper describes the preparation and characterization of a series of O-substituted N-cycloalkylcarbamate derivatives. These compounds were tested as inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). All studied carbamates exhibited moderate inhibitory activity of both cholinesterases with values of IC50 in the range of 36.1–78.6 μM for AChE and 9.8–215.4 μM for BChE, respectively. These values are comparable with those values of inhibition obtained with the established drug rivastigmine. The cytotoxicity of all carbamates was evaluated using standard in vitro test with Jurkat cells. Many of the studied carbamates can be considered as promising compounds for potential medicinal applications with regard to their inhibitory activity as well as negligible cytotoxicity.

Czech name

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Czech description

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Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

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OECD FORD branch

10401 - Organic chemistry

Project

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Continuities

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

Publication year

2017

Confidentiality

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

Name of the periodical

Monatshefte fur Chemie

ISSN

0026-9247

e-ISSN

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Volume of the periodical

148

Issue of the periodical within the volume

12

Country of publishing house

AT - AUSTRIA

Number of pages

11

Pages from-to

"2143–2153"

UT code for WoS article

000415301700014

EID of the result in the Scopus database

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