New group of monoquaternary reactivators of the acetylcholinesterase inhibited by nerve agents

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60162694%3AG44__%2F05%3A00001349" target="_blank" >RIV/60162694:G44__/05:00001349 - 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

New group of monoquaternary reactivators of the acetylcholinesterase inhibited by nerve agents

Popis výsledku v původním jazyce

Reactivators of acetylcholinesterase (AChE; EC 3.1.1.7) are compounds, which are able to treat intoxication with organophosphorus compounds, especially with pesticides or nerve agents. Owing to the fact that there exist no universal "broad-spectrum" reactivator of oranophosphates-inhibited AChE, many laboratories from the world synthesize new AChE reactivators. In our work, there were synthesized five new and three already known quaternary monopyridinium oximes as potential reactivators of AChE inhibited by nerve agents. Potencies to cleave p-nitrophenyl acetate (PNPA), which is commonly used as model substrate of the 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-methylpyridinium iodide). Three newly synthesized oximes achieved similar nuclephilicity at the similar pKa according to 4-PAM, what is very

Název v anglickém jazyce

New group of monoquaternary reactivators of the acetylcholinesterase inhibited by nerve agents

Popis výsledku anglicky

Reactivators of acetylcholinesterase (AChE; EC 3.1.1.7) are compounds, which are able to treat intoxication with organophosphorus compounds, especially with pesticides or nerve agents. Owing to the fact that there exist no universal "broad-spectrum" reactivator of oranophosphates-inhibited AChE, many laboratories from the world synthesize new AChE reactivators. In our work, there were synthesized five new and three already known quaternary monopyridinium oximes as potential reactivators of AChE inhibited by nerve agents. Potencies to cleave p-nitrophenyl acetate (PNPA), which is commonly used as model substrate of the 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-methylpyridinium iodide). Three newly synthesized oximes achieved similar nuclephilicity at the similar pKa according to 4-PAM, what is very

Druh

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

CEP obor

FP - Ostatní lékařské obory

OECD FORD obor

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Projekt

<a href="/cs/project/ONVLAJEP20031" target="_blank" >ONVLAJEP20031: INTOXIKACE - Nové možnosti terapie intoxikací cyklosinem: syntéza a testování nových reaktivátorů acetylcholinesterázy</a><br>

Návaznosti

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

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

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Kód UT WoS článku

000230820000004

EID výsledku v databázi Scopus

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