Design, synthesis and evaluation of genistein-O-alkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease

Design, synthesis and evaluation of scutellarein- O -acetamidoalkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease

“…Generally, the N-2-methoxybenzyl groups indicated stronger inhibitory potency than N-benzyl groups. And the compounds possessing a N-ethyl group showed obviously better AChE inhibitory activity than the compounds with a N-methyl group, which was consistent with the previously reported results in our lab [22,23]. On the other hand, we also investigated the effects of the side chain length on inhibitory ability of AChE, the optimal chain length was four-methylene linker.…”

“…[23] Materials and animals Donepezil was purchased from Eisai China Inc. Scopolamine was purchase from J&K Scientific. light-dark cycle, a temperature and humidity controlled environment with access to food and water ad libitum.…”

“…The determination of AChE and BuChE inhibitory capacity of the compounds were tested by Ellman assay with slight modification, using AChE from 5% rat cortex homogenate or purified AChE from electric eel (Sigma-Aldrich Co.) or BuChE from rat serum [22,23]. The brain homogenate was pre-incubated for 5 min with tetraisopropyl pyrophosphoramide (iso-OMPA, selective inhibitor of Changes in absorbance were detected at 412 nm.…”

Design, Synthesis and Evaluation of Genistein-polyamine Conjugates as Multi-functional Anti-Alzheimer Agents

“…Besides, a number of genistein derivatives have been reported as anti-AD agents in the past years ( Fig. 1) 12,13 . These results indicate that genistein could be used as leading compound for the treatment of AD.…”

Shogaol–huprine hybrids: Dual antioxidant and anticholinesterase agents with β-amyloid and tau anti-aggregating properties

“…8 Usually, the starting point for the design of such compounds is the structure of a known AChE inhibitor, which is linked to an antioxidant pharmacophoric moiety, [11][12][13][14][15][16][17][18] e.g. phenolics and polyphenolics derived fragments.…”