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

Kód výsledku v 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>

Výsledek na webu

<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>

Jazyk výsledku

angličtina

Název v původním jazyce

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

Popis výsledku v původním jazyce

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.

Název v anglickém jazyce

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

Popis výsledku anglicky

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.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

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OECD FORD obor

10401 - Organic chemistry

Projekt

—

Návaznosti

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

Rok uplatnění

2017

Kód důvěrnosti údajů

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

Název periodika

Monatshefte fur Chemie

ISSN

0026-9247

e-ISSN

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Svazek periodika

148

Číslo periodika v rámci svazku

12

Stát vydavatele periodika

AT - Rakouská republika

Počet stran výsledku

11

Strana od-do

"2143–2153"

Kód UT WoS článku

000415301700014

EID výsledku v databázi Scopus

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