Publication details
Trisubstituted 1,3,5-Triazines and Their Effect on BACE1.
| Authors | |
|---|---|
| Year of publication | 2023 |
| Type | Article in Proceedings |
| Conference | Chemistry Proceedings |
| MU Faculty or unit | |
| Citation | |
| Web | https://www.mdpi.com/2673-4583/14/1/48 |
| Doi | http://dx.doi.org/10.3390/ecsoc-27-16111 |
| Keywords | triazinylaminobenzenesulfonamides; Alzheimer’s disease; BACE1; modulation |
| Description | 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 ß-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. |