Synthesis and evaluation of tacrine-huperzine A hybrids as acetylcholinesterase inhibitors of potential interest for the treatment of Alzheimer's disease

Seventeen polycyclic compounds related to tacrine and huperzine A have been prepared as racemic mixtures and tested as acetylcholinesterase (AChE) inhibitors. The conjunctive pharmacomodulation of huperzine A (carbobicyclic substructure) and tacrine (4-aminoquinoline substructure) led to compound 7j...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 1998-04, Vol.6 (4), p.427-440
Hauptverfasser:	Badia, A, Baños, J E, Camps, P, Contreras, J, Görbig, D M, Muñoz-Torrero, D, Simón, M, Vivas, N M
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylcholinesterase - metabolism Alkaloids Alzheimer Disease - drug therapy Animals Cattle Cholinesterase Inhibitors - chemical synthesis Cholinesterase Inhibitors - pharmacology Cholinesterase Inhibitors - therapeutic use Magnetic Resonance Spectroscopy Male Neuromuscular Junction - drug effects Neuroprotective Agents - chemistry Neuroprotective Agents - pharmacology Neuroprotective Agents - therapeutic use Rats Rats, Sprague-Dawley Sesquiterpenes - chemistry Sesquiterpenes - pharmacology Spectrophotometry, Infrared Tacrine - analogs & derivatives Tacrine - pharmacology Tacrine - therapeutic use
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