Nové monokvarterní reaktivátory acetylcholinesterázy inhibované nervovými jedy

Kód výsledku v 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>

Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

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

Popis výsledku v původním jazyce

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

Název v anglickém jazyce

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

Popis výsledku anglicky

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

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

CC - Organická chemie

OECD FORD obor

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Projekt

<a href="/cs/project/GA203%2F01%2F1093" target="_blank" >GA203/01/1093: Vliv elektronové distribuce na reaktivitu oximů vůči esterům</a><br>

Návaznosti

Z - Vyzkumny zamer (s odkazem do CEZ)

Rok uplatnění

2005

Kód důvěrnosti údajů

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

Název periodika

Journal of Enzyme Inhibition and Medicinal Chemistry

ISSN

1475-6366

e-ISSN

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Svazek periodika

20

Číslo periodika v rámci svazku

3

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

5

Strana od-do

233-237

Kód UT WoS článku

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EID výsledku v databázi Scopus

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