Trimethoxycinnamates and Their Cholinesterase Inhibitory Activity
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00027162%3A_____%2F21%3AN0000121" target="_blank" >RIV/00027162:_____/21:N0000121 - isvavai.cz</a>
Alternative codes found
RIV/86652079:_____/21:00543720 RIV/00216275:25310/21:39917740 RIV/61989592:15640/21:73607379
Result on the web
<a href="https://www.mdpi.com/2076-3417/11/10/4691" target="_blank" >https://www.mdpi.com/2076-3417/11/10/4691</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3390/app11104691" target="_blank" >10.3390/app11104691</a>
Alternative languages
Result language
angličtina
Original language name
Trimethoxycinnamates and Their Cholinesterase Inhibitory Activity
Original language description
A series of twelve nature-inspired 3,4,5-trimethoxycinnamates were prepared and characterized. All compounds, including the starting 3,4,5-trimethoxycinnamic acid, were tested for their ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) in vitro; the selectivity index (SI) was also determined. 2-Fluororophenyl (2E)-3-(3,4,5-trimethoxyphenyl)-prop-2-enoate demonstrated the highest SI (1.71) in favor of BChE inhibition. 2-Chlorophenyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate showed the highest AChE-inhibiting (IC50 = 46.18 µM) as well as BChE-inhibiting (IC50 = 32.46 µM) activity with an SI of 1.42. The mechanism of action of the most potent compound was determined by the Lineweaver–Burk plot as a mixed type of inhibition. An in vitro cell viability assay confirmed the insignificant cytotoxicity of the discussed compounds on the two cell lines. Trends between structure, physicochemical properties and activity were discussed.
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
30107 - Medicinal chemistry
Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
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
2021
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
APPLIED SCIENCES-BASEL
ISSN
2076-3417
e-ISSN
2076-3417
Volume of the periodical
11
Issue of the periodical within the volume
10
Country of publishing house
CH - SWITZERLAND
Number of pages
14
Pages from-to
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UT code for WoS article
000662573000001
EID of the result in the Scopus database
2-s2.0-85107275734