Chalcone-based carbamates for Alzheimer's disease treatment

Alzheimer's disease is a still untreatable multifaceted pathology, and drugs able to stop or reverse its progression are urgently needed. In this picture, the recent reformulation of the cholinergic hypothesis renewed the interest for acetylcholinesterase inhibitors. In this paper, a series of...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Future medicinal chemistry 2017-05, Vol.9 (8), p.749-764
Hauptverfasser: Rampa, Angela, Montanari, Serena, Pruccoli, Letizia, Bartolini, Manuela, Falchi, Federico, Feoli, Alessandra, Cavalli, Andrea, Belluti, Federica, Gobbi, Silvia, Tarozzi, Andrea, Bisi, Alessandra
Format: Artikel
Sprache:eng
Schlagworte:
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:Alzheimer's disease is a still untreatable multifaceted pathology, and drugs able to stop or reverse its progression are urgently needed. In this picture, the recent reformulation of the cholinergic hypothesis renewed the interest for acetylcholinesterase inhibitors. In this paper, a series of naturally inspired chalcone-based carbamates was designed to target cholinesterase enzymes and possibly generate fragments endowed with neuroprotective activity . All compounds presented in this study showed nanomolar potency for cholinesterase inhibition. Notably, fragment also displayed an interesting neuroprotective profile. These new derivatives are able to simultaneously modulate different key targets involved in Alzheimer's disease, and could be regarded as promising starting points for the development of disease-modifying drug candidates.
ISSN:1756-8919
1756-8927
DOI:10.4155/fmc-2017-0029