Rational Approach To Discover Multipotent Anti-Alzheimer Drugs

The coupling of two different pharmacophores, each endowed with different biological properties, afforded the hybrid compound lipocrine (7), whose biological profile was markedly improved relative to those of prototypes tacrine and lipoic acid. Lipocrine is the first compound that inhibits the catal...

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Veröffentlicht in:	Journal of medicinal chemistry 2005-01, Vol.48 (2), p.360-363
Hauptverfasser:	Rosini, Michela, Andrisano, Vincenza, Bartolini, Manuela, Bolognesi, Maria L, Hrelia, Patrizia, Minarini, Anna, Tarozzi, Andrea, Melchiorre, Carlo
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylcholinesterase - chemistry Alzheimer Disease - drug therapy Amyloid beta-Peptides - chemistry Antioxidants - chemical synthesis Antioxidants - chemistry Antioxidants - pharmacology Butyrylcholinesterase - chemistry Cell Line Cholinesterase Inhibitors - chemical synthesis Cholinesterase Inhibitors - chemistry Cholinesterase Inhibitors - pharmacology Humans Neurons - cytology Neurons - drug effects Nootropic Agents - chemical synthesis Nootropic Agents - chemistry Nootropic Agents - pharmacology Reactive Oxygen Species - metabolism Structure-Activity Relationship Tacrine - analogs & derivatives Tacrine - chemical synthesis Tacrine - chemistry Tacrine - pharmacology Thioctic Acid - analogs & derivatives Thioctic Acid - chemical synthesis Thioctic Acid - chemistry Thioctic Acid - pharmacology
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Zusammenfassung:	The coupling of two different pharmacophores, each endowed with different biological properties, afforded the hybrid compound lipocrine (7), whose biological profile was markedly improved relative to those of prototypes tacrine and lipoic acid. Lipocrine is the first compound that inhibits the catalytic activity of AChE and AChE-induced amyloid-β aggregation and protects against reactive oxygen species. Thus, it emerged as a valuable pharmacological tool to investigate Alzheimer's disease and as a promising lead compound for new anti-Alzheimer drugs.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm049112h