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New hybrids of tacrine and indomethacin as multifunctional acetylcholinesterase inhibitors

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F21%3A10438556" target="_blank" >RIV/00216208:11160/21:10438556 - isvavai.cz</a>

  • Result on the web

    <a href="https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=2hKduYT2dC" target="_blank" >https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=2hKduYT2dC</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1007/s11696-020-01295-y" target="_blank" >10.1007/s11696-020-01295-y</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    New hybrids of tacrine and indomethacin as multifunctional acetylcholinesterase inhibitors

  • Original language description

    A new series of hybrid compounds were designed, consisting of anti-AChE and BuChE activity components with an anti-inflammatory component. A series of 9-amino-1,2,3,4-tetrahydroacridine and indomethacin derivatives were synthesized. All compounds were created using alkyldiamine with different chain lengths as a linker. Various biological activities were evaluated, including inhibitory activity against AChE and BuChE. The tested compounds showed high inhibitory activities against cholinesterases. The IC(50) values for all compounds ranging from 10 nM to 7 mu M. The potency of inhibition was much higher than well-known AChE and BuChE inhibitors (tacrine and donepezil). Compound3hhad the strongest inhibitory activity; kinetic studies showed it to have a mixed-type of acetylcholinesterase inhibition properties. The cytotoxicity of the newly-synthesized compounds against HepG2 (hepatocarcinoma cells) and EA.hy96 (human vein endothelial cells) cell lines was determined using the MTT and MTS tests. All investigated compounds presented similar cytotoxic activity against HepG2 and EA.hy926 cell line, ranged in micromolar values. Compounds with longer linkers showed higher antioxidant activity. The most active compound was3h. Docking studies confirmed interactions with important regions of AChE and BuChE. Its multifunctional properties, i.e. high activity against AChE and BuChE, antioxidant activity and low cytotoxicity, highlight3has a promising agent for the treatment of AD.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database

  • CEP classification

  • OECD FORD branch

    30104 - Pharmacology and pharmacy

Result continuities

  • Project

  • Continuities

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

Others

  • Publication year

    2021

  • Confidentiality

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

Data specific for result type

  • Name of the periodical

    Chemical Papers

  • ISSN

    2585-7290

  • e-ISSN

  • Volume of the periodical

    75

  • Issue of the periodical within the volume

    1

  • Country of publishing house

    SK - SLOVAKIA

  • Number of pages

    16

  • Pages from-to

    249-264

  • UT code for WoS article

    000553732100001

  • EID of the result in the Scopus database

    2-s2.0-85088841057