Journal of Medicinal Chemistry · 2004 · 226 citations · 11 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoveryNeuropharmacologyAlzheimer DiseaseCholinergic PharmacologyDementia PharmacotherapyLead Compound DesignNeurodegenerative Disease PharmacologyNeurodegenerative Disease PharmacotherapyAlzheimer Disease NeuroprotectionAmyloid Beta AggregationCatalytic ActivityLead Compound IdentificationLipoic Acid ChemistryMedicinal Chemistry ApplicationsPharmacological Treatment Of DementiaReactive Oxygen Species Generation
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.
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A new and rapid colorimetric determination of acetylcholinesterase activity
George L. Ellman, K. Diane Courtney, Valentino Andres et al. · Biochemical Pharmacology · 1961 · 26.9K citations