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Salicylanilide diethyl phosphates as cholinesterases inhibitors

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216275%3A25310%2F15%3A39899767" target="_blank" >RIV/00216275:25310/15:39899767 - isvavai.cz</a>

  • Alternative codes found

    RIV/00216208:11160/15:10312598

  • Result on the web

    <a href="http://dx.doi.org/10.1016/j.bioorg.2014.11.005" target="_blank" >http://dx.doi.org/10.1016/j.bioorg.2014.11.005</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1016/j.bioorg.2014.11.005" target="_blank" >10.1016/j.bioorg.2014.11.005</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Salicylanilide diethyl phosphates as cholinesterases inhibitors

  • Original language description

    Based on the presence of dialkyl phosphate moiety, we evaluated twenty-seven salicylanilide diethyl phosphates (diethyl [2-(phenylcarbamoyl) phenyl] phosphates) for the inhibition of acetylcholinesterase (AChE) from electric eel (Electrophorus electricus L.) and butyrylcholinesterase (BChE) from equine serum. Ellman's spectrophotometric method was used. The inhibitory activity (expressed as IC50 values) was compared with that of the established drugs galantamine and rivastigmine. Salicylanilide diethyl phosphates showed significant activity against both cholinesterases with IC50 values from 0.903 to 86.3 mu M. IC(50)s for BChE were comparatively lower than those obtained for AChE. All of the investigated compounds showed higher inhibition of AChE than rivastigmine, and six of them inhibited BChE more effectively than both rivastigmine and galantamine. In general, derivatives of 4-chlorosalicylic acid showed enhanced activity when compared to derivatives of 5-halogenated salicylic acids, especially against BChE. The most effective inhibitor of AChE was O-{5-chloro-2-[(3-bromophenyl) carbamoyl] phenyl} O, O-diethyl phosphate with IC50 of 35.4 mu M, which is also one of the most potent inhibitors of BChE. O-{5-Chloro-2-[( 3,4-dichlorophenyl) carbamoyl] phenyl} O, O-diethyl phosphate exhibited in vitro the strongest inhibition of BChE (0.90 mu M). Salicylanilide diethyl phosphates act as pseudo-irreversible cholinesterases inhibitors.

  • 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

    Result was created during the realization of more than one project. More information in the Projects tab.

  • Continuities

    S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Others

  • Publication year

    2015

  • Confidentiality

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

Data specific for result type

  • Name of the periodical

    Bioorganic Chemistry

  • ISSN

    0045-2068

  • e-ISSN

  • Volume of the periodical

    58

  • Issue of the periodical within the volume

    February

  • Country of publishing house

    US - UNITED STATES

  • Number of pages

    5

  • Pages from-to

    48-52

  • UT code for WoS article

    000349086500005

  • EID of the result in the Scopus database