New Multifunctional Agents for Potential Alzheimer's Disease Treatment Based on Tacrine Conjugates with 2-Arylhydrazinylidene-1,3-Diketones.

ABSTRACT: Alzheimer's disease (AD) is considered a modern epidemic because of its increasing prevalence worldwide and serious medico-social consequences, including the economic burden of treatment and patient care. The development of new effective therapeutic agents for AD is one of the most urgent and challenging tasks. To address this need, we used an aminoalkylene linker to combine the well-known anticholinesterase drug tacrine with antioxidant 2-tolylhydrazinylidene-1,3-diketones to create 3 groups of hybrid compounds as new multifunctional agents with the potential for AD treatment. Lead compounds of the new conjugates effectively inhibited acetylcholinesterase (AChE, IC₅₀ 0.24-0.34 µM) and butyrylcholinesterase (BChE, IC₅₀ 0.036-0.0745 µM), with weak inhibition of off-tar

SUBMITTER: Elkina NA 

PROVIDER: S-EPMC9687805 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature