Article
Novel Levetiracetam Derivatives That Are Effective against the Alzheimer-like Phenotype in Mice: Synthesis, in Vitro, ex Vivo, and in Vivo Efficacy Studies.
Journal of medicinal chemistry - 13 Aug 2015
Sola Irene, Aso Ester, Frattini Daniela, López-González Irene, Espargaró Alba, Sabaté Raimon, Di Pietro Ornella, Luque F Javier, Clos M Victòria, Ferrer Isidro, Muñoz-Torrero Diego
Abstract excerpt
We have synthesized a series of heptamethylene-linked levetiracetam-huprine and levetiracetam-(6-chloro)tacrine hybrids to hit amyloid, tau, and cholinergic pathologies as well as β-amyloid (Aβ)-induced epileptiform activity, some of the mechanisms that eventually lead to cognitive deficits in Alzheimer's disease patients. These hybrids are potent inhibitors of human acetylcholinesterase and butyrylcholinesterase...
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