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@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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