Monooxime bispyridinium reactivators bearing xylene linker synthesis and in vitro evaluation on model of organophosphate-inhibited acetylcholinesterase

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60162694%3AG44__%2F16%3A43875596" target="_blank" >RIV/60162694:G44__/16:43875596 - isvavai.cz</a>

Alternative codes found

RIV/00179906:_____/16:10324106 RIV/62690094:18470/16:50004700 RIV/00216208:11160/16:10324106

Result on the web

<a href="http://www.eurekaselect.com/135485/article" target="_blank" >http://www.eurekaselect.com/135485/article</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.2174/1573406411666151002125640" target="_blank" >10.2174/1573406411666151002125640</a>

Result language

angličtina

Original language name

Monooxime bispyridinium reactivators bearing xylene linker synthesis and in vitro evaluation on model of organophosphate-inhibited acetylcholinesterase

Original language description

Nine novel mono-oxime reactivators bearing xylene linker were synthesized in an effort to improve previously prepared xylene bisoximes and monocarbamoyl-monooximes. The novel compounds were tested in vitro on the model of tabun-, paraoxon-, methylparaoxon- and DFP-inhibited human erythrocyte AChE. Their reactivation ability was compared to pralidoxime, asoxime, obidoxime and two previously prepared xylene linked bisoximes (K107, K108). All compounds showed minimal reactivation of tabun-inhibited AChE at selected concentration scale. This finding was explained by molecular modelling study. Bisoximes obidoxime and K108 resulted as the best reactivators for paraoxon-, methylparaoxon-and DFP-inhibited AChE. The loss of non-oxime moiety lead to the loss of reactivation ability within the novel compounds. Though the novel reactivators did not exceed previously known compounds, they confirmed former SAR findings for xylene-linked AChE reactivators.

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

Result was created during the realization of more than one project. More information in the Projects tab.

Continuities

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year

2016

Confidentiality

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

Name of the periodical

Medicinal Chemistry

ISSN

1573-4064

e-ISSN

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Volume of the periodical

12

Issue of the periodical within the volume

4

Country of publishing house

AE - UNITED ARAB EMIRATES

Number of pages

9

Pages from-to

362-370

UT code for WoS article

000376450400006

EID of the result in the Scopus database

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