The role of acetylcholinesterase in Alzheimer’s disease: Enzymatic inhibition studies

• Main Author: Bacalhau, P.
• Publication Date: 2014
• Other Authors: Marques, C., Martins, M.R., Caldeira, A.T., Burke, A.
• Format: Article
• Language: eng
• Source: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
• Download full: http://hdl.handle.net/10174/12912
• topic: Alzheimer’s disease; acetylcholinesterase; reversible inhibitors; quinolinone derivatives; indole derivatives

Alzheimer’s disease (AD) is the most common form of dementia and causes a progressive and irreversible neurodegeneration. It is related with loss of cholinergic function, which affects memory, learning and behavior [1]. Neurophathologically, AD is characterized by the presence of beta-amyloid plaques (A ) and neurofibrillary tangles (NFT) [2] and consequent degeneration of the basal forebrain cholinergic neurons [3]. The loss of cholinergic neurons leads to the progressive reduction of acetylcholine (ACh) in the brain and resulting cognitive impairment in AD [3]. As such, the enzyme acetylcholinesterase (AChE) has been one of the prime targets in search for a treatment for AD, which uses reversible inhibitors of AChE, in order to increase levels of acetylcholine (ACh) in the brain [4]. In the present study a small library of quinolinone and indole derivatives was screened for their eeAChE inhibitory activity using the Ellman method.