Synthesis, characterization and biological evaluation of esterderivatives of 4-(diethylamino) salicylaldehyde cholinesterase and tyrosinase inhibitors
Yükleniyor...
Tarih
2021
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
INESEG Yayıncılık
Erişim Hakkı
info:eu-repo/semantics/openAccess
Özet
Alzheimer's disease, one of the diseases that still has no a specific therapy, has become amajor public health issue owing to the increasing population of the elderly, particularly in richcountries. Inhibitory of cholinesterase enzymes (acetylcholinesterase (AChE) and butyrylcholinesterase(BChE), which hydrolyze acetylcholine (ACh) and butyrylcholine (BCh) neurotransmitters, haverecently become a choice for the therapy of this disease. Therefore, there is currently a great demandfor 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 andstructurally illuminated with FT-IR, 1H- and 13C NMR spectroscopy. The inhibitory properties of thesynthesized 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 thangalanthamine (73.83±0.25 %inhibition) employed as standard. Compound 3 showed significantinhibitory effect against tyrosinase with 87.73±0.22 % inhibition, which is better than kojic acid utilizedas 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.
Açıklama
Anahtar Kelimeler
Esters, Acetylcholinesterase, Butyrylcholinesterase, Tyrosinase
Kaynak
Middle East Journal of Science
WoS Q Değeri
Scopus Q Değeri
Cilt
7
Sayı
2
Künye
Çakmak, R., Çınar, E., Başaran, E. ve Boğa, M. (2021). Synthesis, characterization and biological evaluation of esterderivatives of 4-(diethylamino) salicylaldehyde cholinesterase and tyrosinase inhibitors. Middle East Journal of Science, 7(2), 137-144.
