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

Abstract

Alzheimer's Disease (AD), 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 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. A series of ester derivatives of 4-(diethylamino)salicylaldehyde 1-5 were successfully prepared in present work, and structurally illuminated with FT-IR, 1H and 13C NMR spectroscopy. The inhibition properties of the title molecules on AChE, BChE, and tyrosinase enzymes were extensively investigated, respectively. Compound 1 indicated potent inhibitory properties against BChE with 87.28±0.87% inhibition better than galantamine (73.83±0.25 %inhibition) employed as standard. Compound 3 showed potent inhibitory effect against tyrosinase with 87.73±0.22 % inhibition, which are better than kojic acid utilized as standard. The obtained results clearly revealed that some of these enzyme inhibitors have the potential to be utilized as potent enzyme inhibitors in the future.

Keywords

• Esters
• Acetylcholinesterase
• Butyrylcholinesterase
• Tyrosinase.

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