SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF ESTER DERIVATIVES OF 4-(DIETHYLAMINO) SALICYLALDEHYDE AS CHOLINESTERASE AND TYROSINASE INHIBITORS

Özet

Alzheimer's disease, one of the diseases that still has no a specific therapy, has become a major public health issue owing to the increasing population of the elderly, particularly in rich countries. Inhibitory of cholinesterase enzymes (acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), which hydrolyze acetylcholine (ACh) and butyrylcholine (BCh) neurotransmitters, have recently become a choice for the therapy of this disease. Therefore, there is currently a great demand for novel enzyme inhibitors with desirable properties for applying in the treatment of AD. In this study, a series of ester derivatives of 4-(diethylamino)salicylaldehyde (1-5) were successfully prepared and structurally illuminated with FT-IR, 1H- and 13C NMR spectroscopy. The inhibitory properties of the synthesized molecules on AChE, BChE, and tyrosinase enzymes were investigated, respectively. Compound 1 indicated potent inhibitory activity against BChE with 87.28±0.87% inhibition better than galanthamine (73.83±0.25 %inhibition) employed as standard. Compound 3 showed significant inhibitory effect against tyrosinase with 87.73±0.22 % inhibition, which is better than kojic acid utilized as standard. The obtained results clearly revealed that some of these molecules have the potential to be used as potent enzyme inhibitor candidates in the future studies.