Bifunctional phenolic-choline conjugates as anti-oxidants and acetylcholinesterase inhibitors

作者: Jaroslav Šebestík , Sérgio M Marques , Pedro L Falé , Susana Santos , Daniela M Arduíno

DOI: 10.3109/14756366.2010.529806

关键词:

摘要: Because of the complex cascade molecular events that can occur in brain an Alzheimer’s disease (AD) patient, therapy this neurodegenerative seems more likely to be achieved by multifunctional drugs. Herein, a new series dual-targeting ligands have been developed and vitro bioevaluated. Their architecture is based on conjugating acetylcholinesterase inhibition anti-oxidant properties one entity. Specifically, naturally occurring phenolic acids with recognized (derivatives caffeic acid, rosmarinic trolox) conjugated choline account for recognition (AChE). The synthesized hybrid compounds evidenced AChE inhibitory capacity micromolar range (rationalized modeling studies) good antioxidant properties. effects human neuroblastoma cells, previously treated beta-amyloid peptides 1-methyl-4-phenylpyridinium ion neurotoxins (to simul...

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