The aim of this work was to investigate the new effective agents candidate for treatment of the Alzheimer's disease. So, a series of new and highly active acetylcholinesterase inhibitors derived from hydroxyquinoline ester containing amino acid were synthesized. Antibacterial activities of the molecules were studied by the well-diffusion method against Listeria monocytogenes 4b, Staphylococcus aureus, Escherichia coli, Salmonella typhi H, Brucella abortus, Staphylococcus epidermis sp., Micrococcus luteus, Shigella dysenteria type 10, Bacillus cereus, Pseudomonas putida and antifungal activity against Candida albicans. All the synthesized compounds behave as inhibitors against acetylcholinesterase enzyme. CysEs and MetEs show more inhibition potency.