title: Benzofuran-based hybrid compounds for the inhibition of cholinesterase activity, beta amyloid aggregation, and abeta neurotoxicity.
abstract: The complex etiology of Alzheimer's disease (AD) prompts scientists to develop multitarget strategies to combat causes and symptoms. We therefore designed, synthesized, and tested new hybrid molecules linking a benzofuran ring to a N-methyl- N-benzylamine through a heptyloxy chain, affording a series of potential multifunctional drugs for AD. The cholinesterase inhibitory activity was extended to the inhibition of Abeta fibril formation for 1, 3, and 5. Compound 3 showed an additional neuroprotective effect.
authors.affiliation: Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Bologna, Italy.
authors.forename: Stefano
authors.initials: S
authors.lastname: Rizzo
authors.forename: Céline
authors.initials: C
authors.lastname: Rivière
authors.forename: Lorna
authors.initials: L
authors.lastname: Piazzi
authors.forename: Alessandra
authors.initials: A
authors.lastname: Bisi
authors.forename: Silvia
authors.initials: S
authors.lastname: Gobbi
authors.forename: Manuela
authors.initials: M
authors.lastname: Bartolini
authors.forename: Vincenza
authors.initials: V
authors.lastname: Andrisano
authors.forename: Fabiana
authors.initials: F
authors.lastname: Morroni
authors.forename: Andrea
authors.initials: A
authors.lastname: Tarozzi
authors.forename: Jean-Pierre
authors.initials: JP
authors.lastname: Monti
authors.forename: Angela
authors.initials: A
authors.lastname: Rampa
mesh_terms: D000110:Acetylcholinesterase / Q000737:chemistry; D000682:Amyloid / Q000737:chemistry / Q000378:metabolism; D016229:Amyloid beta-Peptides / Q000737:chemistry* / Q000378:metabolism; D001572:Benzofurans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002091:Butyrylcholinesterase / Q000737:chemistry; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D009474:Neurons / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D010446:Peptide Fragments / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000682:Amyloid; D016229:Amyloid beta-Peptides; D001572:Benzofurans; D002800:Cholinesterase Inhibitors; D010446:Peptide Fragments; C074636:amyloid beta-protein (25-35); D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase