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

Abstract

Abstract The condensation of tacrine aminopolymethylene derivatives with diethyl (ethoxymethylidene)malonate led to the new hybrid compounds—conjugates, which were the effective inhibitors of acetylcholinesterase (AChE) (IC50 up to 0.538 μM) and butyrylcholinesterase (IC50 up to 0.0314 μM). They can displace propidium iodide from peripherical anionic site of AChE at the level of the reference drug donepezil and demonstrate a weak antioxidant activity. Conjugates are of interest for further extended research as potential drugs for the Alzheimer’s disease treatment.