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Chasing ChEs-MAO B Multi-Targeting 4-Aminomethyl-7-Benzyloxy-2H-Chromen-2-ones.
Rullo, Mariagrazia; Catto, Marco; Carrieri, Antonio; de Candia, Modesto; Altomare, Cosimo Damiano; Pisani, Leonardo.
Afiliación
  • Rullo M; Department of Pharmacy - Drug Sciences, University of Bari "Aldo Moro", via E. Orabona 4, 70125 Bari, Italy.
  • Catto M; Department of Pharmacy - Drug Sciences, University of Bari "Aldo Moro", via E. Orabona 4, 70125 Bari, Italy.
  • Carrieri A; Department of Pharmacy - Drug Sciences, University of Bari "Aldo Moro", via E. Orabona 4, 70125 Bari, Italy.
  • de Candia M; Department of Pharmacy - Drug Sciences, University of Bari "Aldo Moro", via E. Orabona 4, 70125 Bari, Italy.
  • Altomare CD; Department of Pharmacy - Drug Sciences, University of Bari "Aldo Moro", via E. Orabona 4, 70125 Bari, Italy.
  • Pisani L; Department of Pharmacy - Drug Sciences, University of Bari "Aldo Moro", via E. Orabona 4, 70125 Bari, Italy.
Molecules ; 24(24)2019 Dec 09.
Article en En | MEDLINE | ID: mdl-31835376
ABSTRACT
A series of 4-aminomethyl-7-benzyloxy-2H-chromen-2-ones was investigated with the aim of identifying multiple inhibitors of cholinesterases (acetyl- and butyryl-, AChE and BChE) and monoamine oxidase B (MAO B) as potential anti-Alzheimer molecules. Starting from a previously reported potent MAO B inhibitor (3), we studied single-point modifications at the benzyloxy or at the basic moiety. The in vitro screening highlighted triple-acting compounds (6, 8, 9, 16, 20) showing nanomolar and selective MAO B inhibition along with IC50 against ChEs at the low micromolar level. Enzyme kinetics analysis toward AChE and docking simulations on the target enzymes were run in order to get insight into the mechanism of action and plausible binding modes.
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Inhibidores de la Colinesterasa / Cumarinas / Para-Aminobenzoatos / Inhibidores de la Monoaminooxidasa Límite: Humans Idioma: En Año: 2019 Tipo del documento: Article

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Inhibidores de la Colinesterasa / Cumarinas / Para-Aminobenzoatos / Inhibidores de la Monoaminooxidasa Límite: Humans Idioma: En Año: 2019 Tipo del documento: Article