Conjugates of Tacrine with Aminomethylidene-Substituted Malonates: Synthesis and Biological Evaluation

Abstract The condensation of tacrine aminopolymethylene derivatives with diethyl (ethoxymethylidene)malonate led to the new hybrid compounds—conjugates, which were effective inhibitors acetylcholinesterase (AChE) (IC 50 up 0.538 μM) and butyrylcholinesterase 0.0314 μM). They can displace propidium iodide from peripherical anionic site AChE at level reference drug donepezil demonstrate a weak antioxidant activity. Conjugates are interest for further extended research as potential drugs Alzheimer’s disease treatment.