title: Design, Synthesis, and Evaluation of Donepezil-Like Compounds as AChE and BACE-1 Inhibitors.
abstract: An ecofriendly synthetic pathway for the synthesis of donepezil precursors is described. Alternative energy sources were used for the total synthesis in order to improve yields, regioselectively, and rate of each synthetic step and to reduce the coproduction of waste at the same time. For all products, characterized by an improved structural rigidity respect to donepezil, the inhibitor activity on AChE, the selectivity vs BuChE, the side-activity on BACE-1, and the effect on SHSY-5Y neuroblastoma cells viability were tested. Two potential new lead compounds for a dual therapeutic strategy against Alzheimer's disease were envisaged.
authors.affiliation: Dipartimento di Scienze della Salute, Università degli Studi della Magna Græcia Viale Europa , 88100 Loc. Germaneto (CZ), Italy.
authors.forename: Paola
authors.initials: P
authors.lastname: Costanzo
authors.affiliation: Dipartimento di Scienze della Salute, Università degli Studi della Magna Græcia Viale Europa , 88100 Loc. Germaneto (CZ), Italy.
authors.forename: Luca
authors.initials: L
authors.lastname: Cariati
authors.affiliation: Dipartimento di Bioscienze e Territorio, Università del Molise , Contrada Fonte Lappone, 86090 Pesche (IS), Italy.
authors.forename: Doriana
authors.initials: D
authors.lastname: Desiderio
authors.affiliation: Dipartimento di Scienze Motorie e del Benessere, Università di Napoli "Parthenope", Via Medina 40, 80133 Napoli, Italy; CEINGE, Biotecnologie Avanzate, S.C. a R.L., Via G. Salvatore 486, 80145 Napoli, Italy.
authors.forename: Roberta
authors.initials: R
authors.lastname: Sgammato
authors.affiliation: Dipartimento di Scienze Motorie e del Benessere, Università di Napoli "Parthenope" , Via Medina 40, 80133 Napoli, Italy.
authors.forename: Anna
authors.initials: A
authors.lastname: Lamberti
authors.affiliation: Dipartimento di Scienze Motorie e del Benessere, Università di Napoli "Parthenope", Via Medina 40, 80133 Napoli, Italy; CEINGE, Biotecnologie Avanzate, S.C. a R.L., Via G. Salvatore 486, 80145 Napoli, Italy.
authors.forename: Rosaria
authors.initials: R
authors.lastname: Arcone
authors.affiliation: Dipartimento di Scienze della Salute, Università degli Studi della Magna Græcia Viale Europa , 88100 Loc. Germaneto (CZ), Italy.
authors.forename: Raffaele
authors.initials: R
authors.lastname: Salerno
authors.affiliation: Dipartimento di Chimica e Tecnologie Chimiche, Università della Calabria , Via P. Bucci 12 C, 87037 Arcavacata di Rende (CS), Italy.
authors.forename: Monica
authors.initials: M
authors.lastname: Nardi
authors.affiliation: Dipartimento di Scienze Motorie e del Benessere, Università di Napoli "Parthenope", Via Medina 40, 80133 Napoli, Italy; CEINGE, Biotecnologie Avanzate, S.C. a R.L., Via G. Salvatore 486, 80145 Napoli, Italy.
authors.forename: Mariorosario
authors.initials: M
authors.lastname: Masullo
authors.affiliation: Dipartimento di Scienze della Salute, Università degli Studi della Magna Græcia Viale Europa , 88100 Loc. Germaneto (CZ), Italy.
authors.forename: Manuela
authors.initials: M
authors.lastname: Oliverio
keywords: Alzheimer’s disease; acethylcholinesterase; aldol condensation; donepezil analogues; indanones