Synthesis and pharmacology evaluation of novel 1-benzyl-n-(4-(4-arylpiperazin-1-yl)phenyl)piperidin-4-carboxamides, as potential acetylcholinesterase inhibitors

Abstract

Alzheimer’s disease (AD) is a neurodegenerative disease which affects over 50 milion people worldwide.1) AD mainly affects people ages 65 and above. Symptoms are memory loss, decline in learning capacity, and language problems. One of currently available treatments for Alzheimer's disease consists of Cholinesterase (ChEIs) inhibitors, which raise acetylcholine levels in the brain. The drugs currently approved by the FDA for this purpose are donepezil, rivastigmine and galantamine. As a part of our research we designed and synthesized seven novel compounds (6a-g) as potential acetylcholinesterase inhibitors (AChEIs). The compounds contain N-benzyl piperidine moiety, which is common in many inhibitors including donepezil,2) and N-aryl piperazine moieties.