Arylaminopropanone derivatives as potential cholinesterase inhibitors: Synthesis, docking study and biological evaluation
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F86652079%3A_____%2F20%3A00524494" target="_blank" >RIV/86652079:_____/20:00524494 - isvavai.cz</a>
Alternative codes found
RIV/00216224:14160/20:00116638 RIV/62157124:16370/20:43878575
Result on the web
<a href="https://www.mdpi.com/1420-3049/25/7/1751" target="_blank" >https://www.mdpi.com/1420-3049/25/7/1751</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3390/molecules25071751" target="_blank" >10.3390/molecules25071751</a>
Alternative languages
Result language
angličtina
Original language name
Arylaminopropanone derivatives as potential cholinesterase inhibitors: Synthesis, docking study and biological evaluation
Original language description
Neurodegenerative diseases in which the decrease of the acetylcholine is observed are growing worldwide. In the present study, a series of new arylaminopropanone derivatives with N-phenylcarbamate moiety (1-16) were prepared as potential acetylcholinesterase and butyrylcholinesterase inhibitors. In vitro enzyme assays were performed, the results are expressed as a percentage of inhibition and the IC50 values. The inhibitory activities were compared with reference drugs galantamine and rivastigmine showing piperidine derivatives (1-3) as the most potent. A possible mechanism of action for these compounds was determined from a molecular modelling study by using combined techniques of docking, molecular dynamics simulations and quantum mechanics calculations.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30104 - Pharmacology and pharmacy
Result continuities
Project
<a href="/en/project/LM2018123" target="_blank" >LM2018123: CzeCOS</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2020
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Molecules
ISSN
1420-3049
e-ISSN
1420-3049
Volume of the periodical
25
Issue of the periodical within the volume
7
Country of publishing house
CH - SWITZERLAND
Number of pages
17
Pages from-to
molecules25071751
UT code for WoS article
000531833400276
EID of the result in the Scopus database
2-s2.0-85083258400