Monooxime-monocarbamoyl bispyridinium xylene linked reactivators of acetylcholinesterase - synthesis, in vitro and toxicity evaluation, and docking studies

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60162694%3AG44__%2F10%3A00002295" target="_blank" >RIV/60162694:G44__/10:00002295 - isvavai.cz</a>

Alternative codes found

RIV/44555601:13440/10:00005548 RIV/00216208:11160/10:00300569

Result on the web

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DOI - Digital Object Identifier

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Result language

angličtina

Original language name

Monooxime-monocarbamoyl bispyridinium xylene linked reactivators of acetylcholinesterase - synthesis, in vitro and toxicity evaluation, and docking studies

Original language description

New series of twenty six monooxime-monocarbamoyl xylene linked bispyridinium compounds was prepared. The known reactivators (pralidoxime, HI-6, obidoxime, trimedoxime, methoxime, K107, K108 and K203) and the prepared compounds were tested in vitro on a model of tabun- and paraoxon-, methylparaoxon- and DFP-inhibited human erythrocyte acetylcholinesterase. Although their reactivation ability against tabun did not exceed the previously known compounds, some newly prepared compounds showed promising ability in reactivation of pesticide-inhibited AChE. The acute toxicity of the novel compounds was determined. The docking study for tabun-inhibited AChE was performed for 3 compounds of interest. The structure-activity relationship (SAR) study confirmed apparent influence of xylene linkage and carbamoyl moiety on the reactivation ability and toxicity.

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

Z - Vyzkumny zamer (s odkazem do CEZ)

Publication year

2010

Confidentiality

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

Name of the periodical

ChemMedChem

ISSN

1860-7179

e-ISSN

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Volume of the periodical

5

Issue of the periodical within the volume

2

Country of publishing house

DE - GERMANY

Number of pages

8

Pages from-to

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UT code for WoS article

000274538600009

EID of the result in the Scopus database

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