Abstract
Cholinesterases (ChEs) play a vital role in the regulation of cholinergic transmission. The inhibition of ChEs is considered to be involved in increasing acetylcholine level in the brain and thus has been implicated in the treatment of Alzheimer’s disease. We have designed and synthesized a series of novel indole derivatives and screened them for inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Most of the tested compounds exhibited inhibitory activity against AChE and BChE. Among them 4f and 6e showed the highest AChE inhibitory activity with IC50 91.21±0.06 and 68.52±0.04 μM, respectively. However compound 5a exhibited the highest inhibitory activity against BChE (IC50 55.21±0.12 μM).
Highlights
Alzheimer’s disease (AD), the most common form of neurodegenerative senile dementia, is associated with selective loss of cholinergic neurons and reduced level of acetylcholine neurotransmitter
The illness is characterized by memory deficit and progressive impairment of cognitive functions [1]
It has been revealed that an estimated 35.6 million people worldwide live with dementia [2]
Summary
Alzheimer’s disease (AD), the most common form of neurodegenerative senile dementia, is associated with selective loss of cholinergic neurons and reduced level of acetylcholine neurotransmitter. The current therapeutic approach exploits the enhancement of the central cholinergic function [13] to increase the acetylcholine levels in the brain. Based on the promising nature of the indole analogues, we have designed and synthesized a series of new indolemoiety containing compounds (5a-5c, 6a-6e) along with known (4a-4g) and screened them for inhibition of AChE and BChE. This communication deals with the synthesis of these compounds and their biological and docking studies
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