SAR Study on Reactivators of Ethyl-Paraoxon Inhibited Acetylcholinesterase

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00179906%3A_____%2F12%3A10124634" target="_blank" >RIV/00179906:_____/12:10124634 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/60162694:G44__/12:43874561 RIV/00216208:11160/12:10124634

Výsledek na webu

<a href="http://www.benthamdirect.org/pages/b_viewarticle.php?articleID=3177425" target="_blank" >http://www.benthamdirect.org/pages/b_viewarticle.php?articleID=3177425</a>

DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

SAR Study on Reactivators of Ethyl-Paraoxon Inhibited Acetylcholinesterase

Popis výsledku v původním jazyce

The current treatment of organophosphorus compounds induced intoxication consists of combined administration of anticholinergic drug, oxime reactivator and anticonvulsant. Oxime reactivators are causal treatment of organophosphorus intoxication and theyare able to cleave OP moiety from the molecule of inhibited acetylcholinesterase. Unfortunately, none of the currently used oximes is sufficiently effective against all nerve agents and pesticides. Thus, finding of new potent acetylcholinesterase reactivators is necessary. In this study, the reactivation efficacy of three series of novel bisquaternary reactivators with prop-1,3-diyl, but-1,4-diyl and but-2-ene-1,4-diyl linker against paraoxon inhibited acetylcholinesterase in vitro is presented. The obtained results were compared to the commercially used reactivators (pralidoxime, trimedoxime, obidoxime, methoxime, asoxime). Some newly prepared compounds showed promising ability of paraoxon in vitro reactivation, even in human attainabl

Název v anglickém jazyce

SAR Study on Reactivators of Ethyl-Paraoxon Inhibited Acetylcholinesterase

Popis výsledku anglicky

The current treatment of organophosphorus compounds induced intoxication consists of combined administration of anticholinergic drug, oxime reactivator and anticonvulsant. Oxime reactivators are causal treatment of organophosphorus intoxication and theyare able to cleave OP moiety from the molecule of inhibited acetylcholinesterase. Unfortunately, none of the currently used oximes is sufficiently effective against all nerve agents and pesticides. Thus, finding of new potent acetylcholinesterase reactivators is necessary. In this study, the reactivation efficacy of three series of novel bisquaternary reactivators with prop-1,3-diyl, but-1,4-diyl and but-2-ene-1,4-diyl linker against paraoxon inhibited acetylcholinesterase in vitro is presented. The obtained results were compared to the commercially used reactivators (pralidoxime, trimedoxime, obidoxime, methoxime, asoxime). Some newly prepared compounds showed promising ability of paraoxon in vitro reactivation, even in human attainabl

Druh

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

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

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Projekt

<a href="/cs/project/ME09086" target="_blank" >ME09086: Vývoj nových antidotních prostředků proti organofosforovým pesticidům</a><br>

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2012

Kód důvěrnosti údajů

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

Název periodika

Letters in Drug Design and Discovery

ISSN

1570-1808

e-ISSN

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Svazek periodika

9

Číslo periodika v rámci svazku

6

Stát vydavatele periodika

NL - Nizozemsko

Počet stran výsledku

8

Strana od-do

587-594

Kód UT WoS článku

000308697100005

EID výsledku v databázi Scopus

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