Rational approach to discover multipotent anti-Alzheimer drugs.

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Rosini M, Andrisano V, Bartolini M, Bolognesi ML, Hrelia P, Minarini A, Tarozzi A, Melchiorre C

Rational approach to discover multipotent anti-Alzheimer drugs.

J Med Chem. 2005 Jan 27;48(2):360-3.

PubMed ID

15658850 [ View in PubMed

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Abstract

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-beta 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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Tacrine	Acetylcholinesterase	IC 50 (nM)	424	8	37	Details