title: Substituted 2-aminothiazoles are exceptional inhibitors of neuronal degeneration in tau-driven models of Alzheimer's disease.
abstract: A novel series of 2-aminothiazoles with strong protection in an Alzheimer's disease (AD) model comprising tau-induced neuronal toxicity is disclosed. These derivatives can be synthesized in one-pot and a small SAR of the substitution within these series afforded several compounds that counteracted tau-induced cell toxicity at nanomolar concentrations. These congeners therefore have strong potential as possible treatment for Alzheimer's disease and other related tauopathies.
authors.affiliation: Laboratory for Medicinal Chemistry, Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat, Leuven, Belgium.
authors.forename: Irene
authors.initials: I
authors.lastname: Lagoja
authors.forename: Christophe
authors.initials: C
authors.lastname: Pannecouque
authors.forename: Gerard
authors.initials: G
authors.lastname: Griffioen
authors.forename: Stefaan
authors.initials: S
authors.lastname: Wera
authors.forename: Veronica Maria
authors.initials: VM
authors.lastname: Rojasdelaparra
authors.forename: Arthur
authors.initials: A
authors.lastname: Van Aerschot
mesh_terms: D000544:Alzheimer Disease / Q000473:pathology*; D002460:Cell Line; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008954:Models, Biological; D009474:Neurons / Q000187:drug effects* / Q000473:pathology; D013844:Thiazoles / Q000737:chemistry / Q000494:pharmacology*; D016875:tau Proteins / Q000502:physiology*
chemical_list: D013844:Thiazoles; D016875:tau Proteins; C004483:2-aminothiazole