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

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.

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

• Original language: English
• Type of outcome: Proceedings paper
• Field of Study: 30104 Pharmacology and pharmacy
• Country of publisher: Switzerland
• Confidentiality degree: is not subject to a state or trade secret
• Publication form: electronic version available online
• WWW: URL
• RIV identification code: RIV/00216224:14160/23:00133486
• Organization unit: Faculty of Pharmacy
• ISSN: 2673-4583
• Doi: http://dx.doi.org/10.3390/ecsoc-27-16111
• Keywords in English: triazinylaminobenzenesulfonamides; Alzheimer’s disease; BACE1; modulation
• Tags: rivok, ÚChL

Abstract

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.