Trimethoxycinnamates and Their Cholinesterase Inhibitory Activity

Kód výsledku v 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>

Nalezeny alternativní kódy

RIV/86652079:_____/21:00543720 RIV/00216275:25310/21:39917740 RIV/61989592:15640/21:73607379

Výsledek na webu

<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>

Jazyk výsledku

angličtina

Název v původním jazyce

Trimethoxycinnamates and Their Cholinesterase Inhibitory Activity

Popis výsledku v původním jazyce

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.

Název v anglickém jazyce

Trimethoxycinnamates and Their Cholinesterase Inhibitory Activity

Popis výsledku anglicky

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.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

30107 - Medicinal chemistry

Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2021

Kód důvěrnosti údajů

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

Název periodika

APPLIED SCIENCES-BASEL

ISSN

2076-3417

e-ISSN

2076-3417

Svazek periodika

11

Číslo periodika v rámci svazku

10

Stát vydavatele periodika

CH - Švýcarská konfederace

Počet stran výsledku

14

Strana od-do

—

Kód UT WoS článku

000662573000001

EID výsledku v databázi Scopus

2-s2.0-85107275734