Trisubstituted 1,3,5-Triazines and Their Effect on BACE1.

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216224%3A14160%2F23%3A00133486" target="_blank" >RIV/00216224:14160/23:00133486 - isvavai.cz</a>

Výsledek na webu

<a href="http://dx.doi.org/10.3390/ecsoc-27-16111" target="_blank" >http://dx.doi.org/10.3390/ecsoc-27-16111</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.3390/ecsoc-27-16111" target="_blank" >10.3390/ecsoc-27-16111</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Trisubstituted 1,3,5-Triazines and Their Effect on BACE1.

Popis výsledku v původním jazyce

Alzheimer’s disease (AD) is a multifactorial neurological disease of unknown etiology that is associated with various risk factors. Various pharmacological approaches targeting distinct mechanisms have been investigated; however, they have not yet achieved disease-modifying effects. A series of nine trisubstituted 1,3,5-triazine-based derivatives was investigated as potential inhibitors of the β-secretase enzyme (beta-site amyloid precursor protein-cleaving enzyme 1, BACE1), one of the key enzymes in the pathogenesis of AD. Although the triazine-based derivatives are reported to be potent BACE1 inhibitors, the compounds discussed in this contribution, at a concentration of 10 µM, demonstrated completely insignificant activity. It is worth noting that methyl (4-{4-[(2,3-dihydroxypropyl)amino]-6-[(4-sulfamoylbenzyl)amino]-1,3,5-triazin-2-yl}piperazin-1-yl)- acetate and 4-({4-chloro-6-[(3-hydroxypropyl)amino]-1,3,5-triazin-2-yl}amino)benzenesulfonamide showed an approximately 9% and 2% inhibition of BACE1 activity, respectively.

Název v anglickém jazyce

Trisubstituted 1,3,5-Triazines and Their Effect on BACE1.

Popis výsledku anglicky

Alzheimer’s disease (AD) is a multifactorial neurological disease of unknown etiology that is associated with various risk factors. Various pharmacological approaches targeting distinct mechanisms have been investigated; however, they have not yet achieved disease-modifying effects. A series of nine trisubstituted 1,3,5-triazine-based derivatives was investigated as potential inhibitors of the β-secretase enzyme (beta-site amyloid precursor protein-cleaving enzyme 1, BACE1), one of the key enzymes in the pathogenesis of AD. Although the triazine-based derivatives are reported to be potent BACE1 inhibitors, the compounds discussed in this contribution, at a concentration of 10 µM, demonstrated completely insignificant activity. It is worth noting that methyl (4-{4-[(2,3-dihydroxypropyl)amino]-6-[(4-sulfamoylbenzyl)amino]-1,3,5-triazin-2-yl}piperazin-1-yl)- acetate and 4-({4-chloro-6-[(3-hydroxypropyl)amino]-1,3,5-triazin-2-yl}amino)benzenesulfonamide showed an approximately 9% and 2% inhibition of BACE1 activity, respectively.

Druh

D - Stať ve sborníku

CEP obor

—

OECD FORD obor

30104 - Pharmacology and pharmacy

Projekt

—

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2023

Kód důvěrnosti údajů

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

Název statě ve sborníku

Chemistry Proceedings

ISBN

—

ISSN

2673-4583

e-ISSN

—

Počet stran výsledku

8

Strana od-do

1-8

Název nakladatele

MDPI

Místo vydání

Basel, Switzerland

Místo konání akce

Basel, Switzerland

Datum konání akce

1. 1. 2023

Typ akce podle státní příslušnosti

WRD - Celosvětová akce

Kód UT WoS článku

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