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.

Basic information

Original name

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

Authors

MAJEROVA, P. (703 Slovakia), I. GERHARDTOVA (703 Slovakia), Eva HAVRÁNKOVÁ (203 Czech Republic, guarantor, belonging to the institution), T. JANKECH (703 Slovakia), A. KOVAC (703 Slovakia) and J. JAMPILEK (203 Czech Republic)

Edition

Basel, Switzerland, Chemistry Proceedings, p. 1-8, 8 pp. 2023

Publisher

MDPI

Other information

Language

English

Type of outcome

Stať ve sborníku

Field of Study

30104 Pharmacology and pharmacy

Country of publisher

Switzerland

Confidentiality degree

není předmětem státního či obchodního tajemství

Publication form

electronic version available online

References:

URL

RIV identification code

RIV/00216224:14160/23:00133486

Organization unit

Faculty of Pharmacy

ISSN

DOI

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

Keywords in English

triazinylaminobenzenesulfonamides; Alzheimer’s disease; BACE1; modulation

Abstract

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 and J. JAMPILEK. Trisubstituted 1,3,5-Triazines and Their Effect on BACE1. Online. In Julio A. Seijas. Chemistry Proceedings. Basel, Switzerland: MDPI, 2023, p. 1-8. ISSN 2673-4583. Available from: 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 and J. JAMPILEK. Trisubstituted 1,3,5-Triazines and Their Effect on BACE1. Online. In Julio A. Seijas. \textit{Chemistry Proceedings}. Basel, Switzerland: MDPI, 2023, p.~1-8. ISSN~2673-4583. Available from: https://dx.doi.org/10.3390/ecsoc-27-16111.

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