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

D 2023

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

MAJEROVA, P., I. GERHARDTOVA, Eva HAVRÁNKOVÁ, T. JANKECH, A. KOVAC et. al.

Základní údaje

Originální název

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

Autoři

MAJEROVA, P. (703 Slovensko), I. GERHARDTOVA (703 Slovensko), Eva HAVRÁNKOVÁ (203 Česká republika, garant, domácí), T. JANKECH (703 Slovensko), A. KOVAC (703 Slovensko) a J. JAMPILEK (203 Česká republika)

Vydání

Basel, Switzerland, Chemistry Proceedings, od s. 1-8, 8 s. 2023

Nakladatel

MDPI

Další údaje

Jazyk

angličtina

Typ výsledku

Stať ve sborníku

Obor

30104 Pharmacology and pharmacy

Stát vydavatele

Švýcarsko

Utajení

není předmětem státního či obchodního tajemství

Forma vydání

elektronická verze "online"

Odkazy

URL

Kód RIV

RIV/00216224:14160/23:00133486

Organizační jednotka

Farmaceutická fakulta

ISSN

DOI

http://dx.doi.org/10.3390/ecsoc-27-16111

Klíčová slova anglicky

triazinylaminobenzenesulfonamides; Alzheimer’s disease; BACE1; modulation

Štítky

rivok, ÚChL

Změněno: 7. 2. 2024 20:32, RNDr. Eva Havránková, Ph.D.

Anotace

V originále

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.

Citovat

MAJEROVA, P., I. GERHARDTOVA, Eva HAVRÁNKOVÁ, T. JANKECH, A. KOVAC a J. JAMPILEK. Trisubstituted 1,3,5-Triazines and Their Effect on BACE1. Online. In Julio A. Seijas. Chemistry Proceedings. Basel, Switzerland: MDPI, 2023, s. 1-8. ISSN 2673-4583. Dostupné z: https://dx.doi.org/10.3390/ecsoc-27-16111.

@inproceedings{2371379,
   author = {Majerova, P. and Gerhardtova, I. and Havránková, Eva and Jankech, T. and Kovac, A. and Jampilek, J.},
   address = {Basel, Switzerland},
   booktitle = {Chemistry Proceedings},
   doi = {http://dx.doi.org/10.3390/ecsoc-27-16111},
   editor = {Julio A. Seijas},
   keywords = {triazinylaminobenzenesulfonamides; Alzheimer’s disease; BACE1; modulation},
   howpublished = {elektronická verze "online"},
   language = {eng},
   location = {Basel, Switzerland},
   pages = {1-8},
   publisher = {MDPI},
   title = {Trisubstituted 1,3,5-Triazines and Their Effect on BACE1.},
   url = {https://www.mdpi.com/2673-4583/14/1/48},
   year = {2023}
}

TY  - JOUR
ID  - 2371379
AU  - Majerova, P. - Gerhardtova, I. - Havránková, Eva - Jankech, T. - Kovac, A. - Jampilek, J.
PY  - 2023
TI  - Trisubstituted 1,3,5-Triazines and Their Effect on BACE1.
PB  - MDPI
CY  - Basel, Switzerland
KW  - triazinylaminobenzenesulfonamides
KW  - Alzheimer’s disease
KW  - BACE1
KW  - modulation
UR  - https://www.mdpi.com/2673-4583/14/1/48
N2  - 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.
ER  -

MAJEROVA, P., I. GERHARDTOVA, Eva HAVRÁNKOVÁ, T. JANKECH, A. KOVAC a J. JAMPILEK. Trisubstituted 1,3,5-Triazines and Their Effect on BACE1. Online. In Julio A. Seijas. \textit{Chemistry Proceedings}. Basel, Switzerland: MDPI, 2023, s.~1-8. ISSN~2673-4583. Dostupné z: https://dx.doi.org/10.3390/ecsoc-27-16111.

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