Molecules, Vol. 23, Pages 2033: Synthesis and Biological Evaluation of New Cholinesterase Inhibitors for Alzheimer ’s Disease

Molecules, Vol. 23, Pages 2033: Synthesis and Biological Evaluation of New Cholinesterase Inhibitors for Alzheimer’s Disease Molecules doi: 10.3390/molecules23082033 Authors: Weiam Hussein Begüm Nurpelin Sağlık Serkan Levent Büşra Korkut Sinem Ilgın Yusuf Özkay Zafer Asım Kaplancıklı Alzheimer’s disease (AD) is a neurodegenerative disorder mostly influencing the elderly, and causes death due to dementia. The main pathogenic feature connected with the progression of this multifactorial disease is the weakening of the cholinergic system in the brain. Cholinesterase (ChE) inhibitors are recognized as one of the choices in the treatment of AD. The inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) were approved as a therapeutic strategy to reduce the symptoms of AD and prevent its progression. The capacity of BChE is not completely known yet; rather, it is accepted to assume a part in a few disorders such as AD. Thus, BChE inhibitors may have a greater role for the treatment of AD in the future. In the present study, 2-(9-acridinylamino)-2-oxoethyl piperazine/piperidine/morpholinecarbodithioate derivatives were synthesized in order to investigate anticholinesterase activity. Eight derivatives demonstrated a specific and promising action against BChE. Furthermore, compound 4n showed inhibitory activity against both enzymes. It was found that the active compounds were well tolerated in the cytotoxicity test. Poss...
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research