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Synthesis, in vitro acetylcholinesterase inhibitory activity and molecular docking of new acridine-coumarin hybrids

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60162694%3AG44__%2F17%3A43889386" target="_blank" >RIV/60162694:G44__/17:43889386 - isvavai.cz</a>

  • Alternative codes found

    RIV/62690094:18470/17:50013673 RIV/00179906:_____/17:10364046

  • Result on the web

    <a href="http://www.sciencedirect.com/science/article/pii/S0141813016328197?via%3Dihub" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0141813016328197?via%3Dihub</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1016/j.ijbiomac.2017.06.006" target="_blank" >10.1016/j.ijbiomac.2017.06.006</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Synthesis, in vitro acetylcholinesterase inhibitory activity and molecular docking of new acridine-coumarin hybrids

  • Original language description

    A novel series of acridine-coumarin hybrids was synthesized and biologically evaluated for their potential inhibitory effect on both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The newly synthesized derivatives 9a-d have shown higher activity against human AChE (hAChE) compared with 7-MEOTA as the standard drug. Among them derivative 9b exhibited the most potent acetylcholinesterase inhibitory activity, with an IC50 value of 5.85 mu M compared with 7-MEOTA (IC50 = 15 mu M). Molecular modelling studies were performed to predict the binding modes of compounds 9b, 9c and 9f with hAChE/hBuChE. (C) 2017 Published by Elsevier B.V.

  • 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

    <a href="/en/project/NV15-30954A" target="_blank" >NV15-30954A: Development of multi-target drugs for Alzheimer´s disease: combination of AChE inhibitor and melatonin derivative</a><br>

  • Continuities

    V - Vyzkumna aktivita podporovana z jinych verejnych zdroju

Others

  • Publication year

    2017

  • Confidentiality

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

Data specific for result type

  • Name of the periodical

    International Journal of Biological Macromolecules

  • ISSN

    0141-8130

  • e-ISSN

  • Volume of the periodical

    104

  • Issue of the periodical within the volume

    Part A

  • Country of publishing house

    NL - THE KINGDOM OF THE NETHERLANDS

  • Number of pages

    6

  • Pages from-to

    333-338

  • UT code for WoS article

    000412959300037

  • EID of the result in the Scopus database

    2-s2.0-85020659867