The potential anticholinesterase characteristics of some thiazole derivatives (2a–2j), including the 5-nitrothiophene moiety, were examined in this work. 1H-NMR, 13C-NMR, and HRMS spectral data used to determine structure compounds. Using a modified Ellman's spectrophotometric approach, each compound was tested for its ability inhibit acetylcholinesterase (AChE) butyrylcholinesterase (BuChE) en...

Galanthamine, physostigmine and 9-amino-1,2,3,4-tetrahydroacridine (tacrine) were evaluated as inhibitors of human acetylcholinesterase activity from samples of postmortem human brain, fresh brain cortex biopsies and human erythrocytes. Acetylcholinesterase activity was most effectively inhibited in all tissues by physostigmine, followed by tacrine and galanthamine. The respective inhibitor con...

Donepezil {(RS)-2-[(1-benzyl-4-piperidyl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one} is a reversible acetylcholinesterase inhibitor and used for treatment of patients with AD (Alzheimer's disease). Recent studies showed that treatment with donepezil reduced production of inflammatory cytokines in PBMCs (peripheral blood mononuclear cells). It was also reported that muscle-derived inflammatory...

Factors such as oxidative stress and reduced acetylcholine level have been implicated in Alzheimer’s disease (AD) pathology and recently there has been a trend towards natural product research to find potential sources of antioxidants and acetylcholinesterase inhibitors in the plants kingdom. Centaurea is a genus with about 500 species world wild, many of them have shown to possess bio...

Background: Endophytic fungi are known as a producer of myriad bioactive natural products, including those originally produced by the host plants. Huperzine A (Hup A), lycopodium alkaloid, which was reported an active acetylcholinesterase inhibitor (AChEI) agent used for treatment Alzheimer’s disease, isolated from medicinal Chinese herbs Huperzia serrata. Moreover, various species endophytic a...