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Synthesis of monooxime-monocarbamoyl bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against tabun - and paraoxon-inhibited acetylcholinesterase

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60162694%3AG44__%2F08%3A00002000" target="_blank" >RIV/60162694:G44__/08:00002000 - isvavai.cz</a>

  • Alternative codes found

    RIV/00216208:11160/08:00109179

  • Result on the web

  • DOI - Digital Object Identifier

Alternative languages

  • Result language

    angličtina

  • Original language name

    Synthesis of monooxime-monocarbamoyl bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against tabun - and paraoxon-inhibited acetylcholinesterase

  • Original language description

    Six AChE monooxime-monocarbamoyl reactivators with an (E)-but-2-ene linker were synthesized using modification of currently known synthetic pathways. Their potency to reactivate AChE inhibited by the nerve agent tabun and insecticide paraoxon was testedin vitro. The reactivation efficacies of pralidoxime, HI-6, obidoxime, K048, K075 and the newly prepared reactivators were compared. According to the results obtained, one reactivator seems to be promising against tabun-inhibited AChE and two reactivators against paraoxon-inhibited AChE. The best results were obtained for bisquaternary substances with at least one oxime group in position four.

  • Czech name

    Syntéza monooximových-monokarbamoylovaných bispyridiniových sloučenin nesoucích (E)-but-2-enový spojovací řetězec a jejich evaluace proti tabunem a paraoxonem inhibované acetylcholinesterase

  • Czech description

    Bylo připraveno šest monooximových-monokarbamoylovaných bispyridiniových sloučenin nesoucích (E)-but-2-enový spojovací řetězec, které byly testovány proti tabunem a paraoxonem inhibované acetylcholinesterase.

Classification

  • Type

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

  • CEP classification

    FP - Other medical fields

  • OECD FORD branch

Result continuities

  • Project

  • Continuities

    Z - Vyzkumny zamer (s odkazem do CEZ)

Others

  • Publication year

    2008

  • Confidentiality

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

Data specific for result type

  • Name of the periodical

    Journal of Enzyme Inhibition and Medicinal Chemistry

  • ISSN

    1475-6366

  • e-ISSN

  • Volume of the periodical

    23

  • Issue of the periodical within the volume

    1

  • Country of publishing house

    GB - UNITED KINGDOM

  • Number of pages

    7

  • Pages from-to

  • UT code for WoS article

    000253122700012

  • EID of the result in the Scopus database