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Benzyl Carbamates of 4-Aminosalicylanilides as Possible BACE1 Modulators
oleh: Petra Majerova, Dominika Pindjakova, Timotej Jankech, Ivana Gerhardtova, Jiri Kos, Andrej Kovac, Josef Jampilek
Format: | Article |
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Diterbitkan: | MDPI AG 2022-11-01 |
Deskripsi
Recently, a series of thirty-eight 4-{[(benzyloxy)carbonyl]amino}-2-hydroxybenzoic acid amides designed as potential acetyl- and butyrylcholinesterase (AChE/BChE) inhibitors were described as potential drugs to alleviate the symptoms of Alzheimer’s disease (AD). Some of these compounds have shown promise for inhibiting either AChE or BChE. Since these compounds are structurally similar to agents inhibiting beta-site amyloid precursor protein cleaving enzyme 1 (BACE1), the aim of the contribution was to verify how our compounds were able to affect this enzyme, which, when inhibited, blocks the formation of amyloid-β, but whose inhibition is associated with significant adverse effects in humans. At a concentration of 10 µM, only benzyl {4-[(4-fluorophenyl)carbamoyl]-3-hydroxyphenyl}carbamate was found to show approximately 28% inhibition of BACE1 activity.