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Kinetics of In Vitro Inhibition of Acetylcholinesterase by Nineteen New Carbamates

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216275%3A25310%2F11%3A39895922" target="_blank" >RIV/00216275:25310/11:39895922 - isvavai.cz</a>

  • Result on the web

    <a href="http://dx.doi.org/10.2174/157340811799860560" target="_blank" >http://dx.doi.org/10.2174/157340811799860560</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.2174/157340811799860560" target="_blank" >10.2174/157340811799860560</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Kinetics of In Vitro Inhibition of Acetylcholinesterase by Nineteen New Carbamates

  • Original language description

    Two series A and B of 12 and 7 new carbamate derivates were tested in vitro as acetylcholinesterase inhibitors. The tests were performed in the batch stirred reactor at 25°C, pH 8, ionic strength 0.11 M and catalytic activity of the enzyme preparation 0.14 U mL-1 of the reaction mixture. The temporal dependences of actual concentrations of acetylcholine, choline and acetic acid were determined by two independent analytical methods, HPLC and pH-stat. For all used inhibitors, the model of competitive irreversible inhibition was valid. The inhibition rate constant k3 and qualified estimation of the absolute acetylcholinesterase concentration in the reaction mixture were calculated. The partition coefficients Kow between n-octanol and water of all used inhibitors were determined. The k3 and Kow values were correlated with the Hammett and Hansch substituent constants and with the calculated docking and binding energies of the reaction between the tested inhibitors and acetylcholinesterase.

  • Czech name

  • Czech description

Classification

  • Type

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

  • CEP classification

    CF - Physical chemistry and theoretical chemistry

  • OECD FORD branch

Result continuities

  • Project

  • Continuities

    Z - Vyzkumny zamer (s odkazem do CEZ)<br>S - Specificky vyzkum na vysokych skolach

Others

  • Publication year

    2011

  • Confidentiality

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

Data specific for result type

  • Name of the periodical

    Current Enzyme Inhibition

  • ISSN

    1573-4080

  • e-ISSN

  • Volume of the periodical

    7

  • Issue of the periodical within the volume

    4

  • Country of publishing house

    NL - THE KINGDOM OF THE NETHERLANDS

  • Number of pages

    8

  • Pages from-to

    236-243

  • UT code for WoS article

  • EID of the result in the Scopus database