RT Journal Article
T1 Pyranopyrazolotacrines as nonneurotoxic, Aβ-anti-aggregating and neuroprotective agents for Alzheimer’s disease
A1 Chioua, Mourad
A1 Pérez Peña, Javier
A1 García Font, Nuria
A1 Moraleda, Ignacio
A1 Iriepa, Isabel
A1 Soriano, Elena
A1 Marco Contelles, José
A1 Oset Gasque, María Jesús
AB Aim: Due to the complex nature of Alzheimer’s disease, there is a renewed search for multipotent, nonhepatotoxic tacrines. Results: This paper describes the synthesis and in vitro biological evaluation of eight new racemic 3-methyl-4-aryl-2,4,6,7,8,9-hexahydropyrazolo[4′,3′:5,6]pyrano[2,3-b]quinolin-5-amines (pyranopyrazolotacrines, PPT) as nonhepatotoxic multipotent tacrine analogs. Among these compounds, PPT4 is the less hepatotoxic in the cell viability assay on HepG2 cells, showing a good neuroprotective effect in the decreased cortical neuron viability induced by oligomycin A/rotenone analysis. PPT4 is a selective and good, noncompetitive EeAChE inhibitor, able to completely inhibit the Aβ1–40 aggregation induced by acetylcholinesterase. Conclusion: A new family of permeable tacrine analogs, have been discovered for the potential treatment of Alzheimer’s disease.
PB Future Science
SN 1756-8919
YR 2015
FD 2015
LK https://hdl.handle.net/20.500.14352/34805
UL https://hdl.handle.net/20.500.14352/34805
LA eng
NO Ministerio de Economía y Competitividad (MINECO)
NO UCM
DS Docta Complutense
RD 14 may 2024