Další formáty:
BibTeX
LaTeX
RIS
@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.
|