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Comparison of Novel Tacrine and 7-MEOTA Derivatives with Aromatic and Alicyclic Residues: Synthesis, Biological Evaluation and Docking Studies

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11110%2F13%3A10144061" target="_blank" >RIV/00216208:11110/13:10144061 - isvavai.cz</a>

  • Alternative codes found

    RIV/60162694:G44__/13:43874846 RIV/00216208:11160/13:10144061 RIV/00179906:_____/13:10144061 RIV/00179906:_____/13:10218292

  • Result on the web

    <a href="http://www.ingentaconnect.com/content/ben/loc/2013/00000010/00000004/art00011" target="_blank" >http://www.ingentaconnect.com/content/ben/loc/2013/00000010/00000004/art00011</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.2174/1570178611310040011" target="_blank" >10.2174/1570178611310040011</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Comparison of Novel Tacrine and 7-MEOTA Derivatives with Aromatic and Alicyclic Residues: Synthesis, Biological Evaluation and Docking Studies

  • Original language description

    Cholinesterase inhibitors play an essential role in the treatment of Alzheimer's disease. Since their first introduction over a decade ago, they are an indispensable part of Alzheimer's disease therapy and remain at the forefront of scientific interest worldwide. In this manuscript new analogs of THA and 7-MEOTA were designed, synthesized, and evaluated for their inhibitory activity against both acetylcholinesterase and butyrylcholinesterase. Cholinergic properties were investigated and quantified withrespect to their side chain residues (aromatic or alicyclic). All synthesized compounds proved to have potent inhibitory activity at micromolar range. Moreover, compound 4 demonstrated promising efficacy and appears to be an ideal candidate for further testing.

  • 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/GAP303%2F11%2F1907" target="_blank" >GAP303/11/1907: Novel inhibitors of acetylcholinesterase derived from 7-MEOTA - potential Alzheimer´s disease drugs</a><br>

  • Continuities

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

Others

  • Publication year

    2013

  • 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 Organic Chemistry

  • ISSN

    1570-1786

  • e-ISSN

  • Volume of the periodical

    10

  • Issue of the periodical within the volume

    4

  • Country of publishing house

    AE - UNITED ARAB EMIRATES

  • Number of pages

    7

  • Pages from-to

    291-297

  • UT code for WoS article

    000318689200010

  • EID of the result in the Scopus database