Synthesis and Biological Evaluation of Novel Tacrine Derivatives and Tacrine-Coumarin Hybrids as Cholinesterase Inhibitors

Kód výsledku v 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>

Nalezeny alternativní kódy

RIV/60162694:G44__/14:43875100

Výsledek na webu

<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>

Jazyk výsledku

angličtina

Název v původním jazyce

Synthesis and Biological Evaluation of Novel Tacrine Derivatives and Tacrine-Coumarin Hybrids as Cholinesterase Inhibitors

Popis výsledku v původním jazyce

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.

Název v anglickém jazyce

Synthesis and Biological Evaluation of Novel Tacrine Derivatives and Tacrine-Coumarin Hybrids as Cholinesterase Inhibitors

Popis výsledku anglicky

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.

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

—

Projekt

<a href="/cs/project/GAP303%2F11%2F1907" target="_blank" >GAP303/11/1907: Nové inhibitory acetylcholinesterasy odvozené od látky 7-MEOTA - potenciální léčiva pro Alzheimerovu nemoc</a><br>

Návaznosti

O - Projekt operacniho programu

Rok uplatnění

2014

Kód důvěrnosti údajů

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

Název periodika

Journal of Medicinal Chemistry

ISSN

0022-2623

e-ISSN

—

Svazek periodika

57

Číslo periodika v rámci svazku

16

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

12

Strana od-do

7073-7084

Kód UT WoS článku

000341121400014

EID výsledku v databázi Scopus

—