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Rational Approach To Discover Multipotent Anti-Alzheimer Drugs

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journal contribution
posted on 27.01.2005 by Michela Rosini, Vincenza Andrisano, Manuela Bartolini, Maria L. Bolognesi, Patrizia Hrelia, Anna Minarini, Andrea Tarozzi, Carlo Melchiorre
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.