Charged pyridinium oximes with thiocarboxamide moiety are equally or less effective reactivators of organophosphate-inhibited cholinesterases compared to analogous carboxamides

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F62690094%3A18470%2F22%3A50019053" target="_blank" >RIV/62690094:18470/22:50019053 - isvavai.cz</a>
Alternative codes found
RIV/00179906:_____/22:10442708
Result on the web
<a href="https://www.tandfonline.com/doi/full/10.1080/14756366.2022.2041628" target="_blank" >https://www.tandfonline.com/doi/full/10.1080/14756366.2022.2041628</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1080/14756366.2022.2041628" target="_blank" >10.1080/14756366.2022.2041628</a>

Result language
angličtina
Original language name
Charged pyridinium oximes with thiocarboxamide moiety are equally or less effective reactivators of organophosphate-inhibited cholinesterases compared to analogous carboxamides
Original language description
The organophosphorus antidotes, so-called oximes, are able to restore the enzymatic function of acetylcholinesterase (AChE) or butyrylcholinesterase (BChE) via cleavage of organophosphate from the active site of the phosphylated enzyme. In this work, the charged pyridinium oximes containing thiocarboxamide moiety were designed, prepared and tested. Their stability and pK(a) properties were found to be analogous to parent carboxamides (K027, K048 and K203). The inhibitory ability of thiocarboxamides was found in low mu M levels for AChE and high mu M levels for BChE. Their reactivation properties were screened on human recombinant AChE and BChE inhibited by nerve agent surrogates and paraoxon. One thiocarboxamide was able to effectively restore function of NEMP- and NEDPA-AChE, whereas two thiocarboxamides were able to reactivate BChE inhibited by all tested organophosphates. These results were confirmed by reactivation kinetics, where thiocarboxamides were proved to be effective, but less potent reactivators if compared to carboxamides.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30108 - Toxicology

Project
<a href="/en/project/GA21-03000S" target="_blank" >GA21-03000S: Modified nucleophiles for reactivation of cholinesterases inhibited by organophosphorus compounds</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year
2022
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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