Benzyl Carbamates of 4-Aminosalicylanilides as Possible BACE1 Modulators

Recently, a series of fifty 4-{[(benzyloxy)carbonyl]amino}-2-hydroxybenzoic acid amides designed as potential acetyl- and butyrylcholinesterase (AChE/BChE) inhibitors have been 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 are able to affect this enzyme, which, when inhibited, blocks the formation of beta-amyloid, but whose inhibition is associated with significant negative effects in humans. At a concentration of 10 µM, only benzyl {4-[(4-fluorophenyl)carbamoyl]-3-hydroxyphenyl}carbamate was found to show approximately 30% inhibition of BACE activity.