VII EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry, Vienna, Avusturya, 27 - 31 Ağustos 2017, ss.349
Alzheimer’s disease (AD) is a neurodegenerative disorder which is characterized by progressive and irreversible
cognitive impairment followed by memory loss [1]. The etiology of AD is still not fully known but reduced
levels of the neurotransmitter acetylcholine (ACh) in the brain is believed to be one of the major causes of
cognitive function damage, loss of memory and other possible symptoms of AD [2]. To date, one of the effective
therapeutic strategies to treat AD is to maintain the levels of ACh by inhibiting the enzyme acetylcholinesterase
(AChE) [3]. AChE and butyrylcholinesterase (BuChE) are the two types of cholinesterase enzyme. They both
play important roles in the regulation of ACh levels. It is reported in the literature that the elevated BuChE may
act as a compensatory mechanism for ACh hydrolysis and ACh regulation may become increasingly dependent
on BuChE as AD progresses [4].On the other hand, oxidative stress has been considered as a mechanism
involved in the pathogenesis of AD. It is important to improve the antioxidant defence system of the brain tissue
against the oxidative stress that has a role in the neurodegenerative diseases [5].In the present study, a series of
piperidine hydrazide-hydrazone derivatives (Fig 1) were synthesized, purified and their structures were identified
by spectroscopic methods. AChE and BuChE inhibitory activities were evaluated in vitro by using colorimetric
Ellman’s method [6]. Some of the compounds displayed selective AChE inhibitory activity while some of the
compounds displayed selectivity against BuChE enzyme. The antioxidant activity of the title compounds were
also tested by DPPH and ABTS methods.