Acetylcholinesterase-Inhibiting Activity of Salicylanilide N-Alkylcarbamates and Their Molecular Docking

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216275%3A25310%2F12%3A39894709" target="_blank" >RIV/00216275:25310/12:39894709 - isvavai.cz</a>

Alternative codes found

RIV/00216208:11160/12:10124283 RIV/62157124:16370/12:43871097

Result on the web

<a href="http://dx.doi.org/10.3390/molecules170910142" target="_blank" >http://dx.doi.org/10.3390/molecules170910142</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.3390/molecules170910142" target="_blank" >10.3390/molecules170910142</a>

Result language

angličtina

Original language name

Acetylcholinesterase-Inhibiting Activity of Salicylanilide N-Alkylcarbamates and Their Molecular Docking

Original language description

A series of twenty-five novel salicylanilide N-alkylcarbamates were investigated as potential acetylcholinesterase inhibitors. The compounds were tested for their ability to inhibit acetylcholinesterase (AChE) from electric eel (Electrophorus electricusL.). Experimental lipophilicity was determined, and the structure-activity relationships are discussed. The mode of binding in the active site of AChE was investigated by molecular docking. All the discussed compounds expressed significantly higher AChEinhibitory activity than rivastigmine and slightly lower than galanthamine. Disubstitution by chlorine in C-(3,C-4)' of the aniline ring and the optimal length of hexyl-undecyl alkyl chains in the carbamate moiety provided the most active AChE inhibitors. Monochlorination in C-(4)' exhibited slightly more effective AChE inhibitors than in C-(3)'. Generally it can be stated that compounds with higher lipophilicity showed higher inhibition, and the activity of the compounds is strongly dep

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

FR - Pharmacology and apothecary chemistry

OECD FORD branch

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Project

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Continuities

S - Specificky vyzkum na vysokych skolach

Publication year

2012

Confidentiality

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

Name of the periodical

Molecules

ISSN

1420-3049

e-ISSN

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Volume of the periodical

17

Issue of the periodical within the volume

9

Country of publishing house

CH - SWITZERLAND

Number of pages

17

Pages from-to

10142-10158

UT code for WoS article

000309269700013

EID of the result in the Scopus database

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