A new group of monoquaternary reactivators of acetylcholinesterase inhibited by nerve agents

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22310%2F05%3A00013840" target="_blank" >RIV/60461373:22310/05:00013840 - isvavai.cz</a>
Result on the web
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DOI - Digital Object Identifier
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Result language
angličtina
Original language name
A new group of monoquaternary reactivators of acetylcholinesterase inhibited by nerve agents
Original language description
Reactivators of acetylcholinesterase (AChE; EC 3.1.1.7) are able to treat intoxication by organophosphorus compounds,especially with pesticides or nerve agents. Owing to the fact that there exists no universal #broad-spectrum# reactivator oforganophosphates-inhibited AChE, many laboratories have synthesized new AChE reactivators. Here, we synthesized fivenew and three previously known quaternary monopyridinium oximes as potential reactivators of AChE inhibited by nerveagents. Potencies to cleave p-nitrophenyl acetate (PNPA), which is commonly used as a model substrate of nerve agents, were measured. Their cleaving potencies were compared with 4-PAM (4-hydroxyiminomethyl-1-methylpyridinium iodide), which is derived from the structure of the currently used AChE-reactivator 2-PAM (2-hydroxyiminomethyl-1-methylpyridiniumiodide). Three newly synthesized oximes achieved similar nucleophilicity at the similar pKa according to 4-PAM, which is very promising for using these derivatives as AChE
Czech name
Nové monokvarterní reaktivátory acetylcholinesterázy inhibované nervovými jedy
Czech description
Byly sytetizovány nové typy kvarterních pyridiniových ketoximů, jejichž účinnost byla testována na modelových substrátech.

Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
CC - Organic chemistry
OECD FORD branch
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Project
<a href="/en/project/GA203%2F01%2F1093" target="_blank" >GA203/01/1093: The effect of electron distribution on the oxime reactivity towards esters</a><br>
Continuities
Z - Vyzkumny zamer (s odkazem do CEZ)

Publication year
2005
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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