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SAR Study on Reactivators of Ethyl-Paraoxon Inhibited Acetylcholinesterase

The result's identifiers

  • Result code in 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>

  • Alternative codes found

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

  • Result on the web

    <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

Alternative languages

  • Result language

    angličtina

  • Original language name

    SAR Study on Reactivators of Ethyl-Paraoxon Inhibited Acetylcholinesterase

  • Original language description

    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

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

  • CEP classification

    FR - Pharmacology and apothecary chemistry

  • OECD FORD branch

Result continuities

  • Project

    <a href="/en/project/ME09086" target="_blank" >ME09086: Development of novel antidotal treatment against organophosphorus pesticides</a><br>

  • Continuities

    I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Others

  • Publication year

    2012

  • Confidentiality

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

Data specific for result type

  • Name of the periodical

    Letters in Drug Design and Discovery

  • ISSN

    1570-1808

  • e-ISSN

  • Volume of the periodical

    9

  • Issue of the periodical within the volume

    6

  • Country of publishing house

    NL - THE KINGDOM OF THE NETHERLANDS

  • Number of pages

    8

  • Pages from-to

    587-594

  • UT code for WoS article

    000308697100005

  • EID of the result in the Scopus database