Synthesis and Biological Evaluation of Novel Tacrine Derivatives and Tacrine-Coumarin Hybrids as Cholinesterase Inhibitors
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00179906%3A_____%2F14%3A10272047" target="_blank" >RIV/00179906:_____/14:10272047 - isvavai.cz</a>
Alternative codes found
RIV/60162694:G44__/14:43875100
Result on the web
<a href="http://dx.doi.org/10.1021/jm5008648" target="_blank" >http://dx.doi.org/10.1021/jm5008648</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1021/jm5008648" target="_blank" >10.1021/jm5008648</a>
Alternative languages
Result language
angličtina
Original language name
Synthesis and Biological Evaluation of Novel Tacrine Derivatives and Tacrine-Coumarin Hybrids as Cholinesterase Inhibitors
Original language description
A series of novel tacrine derivatives and tacrine-coumarin heterodimers were designed, synthesized, and biologically evaluated for their potential inhibitory effect on both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Of these compounds, tacrine-coumarin heterodimer 7c and tacrine derivative 6b were found to be the most potent inhibitors of human AChE (hAChE), demonstrating IC50 values of 0.0154 and 0.0263 ?M. Ligands 6b, 6c, and 7c exhibited the highest levels of inhibitory activity against human BuChE (hBuChE), demonstrating IC50 values that range from 0.228 to 0.328 ?M. Docking studies were performed in order to predict the binding modes of compounds 6b and 7c with hAChE/hBuChE.
Czech name
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Czech description
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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
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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
O - Projekt operacniho programu
Others
Publication year
2014
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Journal of Medicinal Chemistry
ISSN
0022-2623
e-ISSN
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Volume of the periodical
57
Issue of the periodical within the volume
16
Country of publishing house
US - UNITED STATES
Number of pages
12
Pages from-to
7073-7084
UT code for WoS article
000341121400014
EID of the result in the Scopus database
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