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Novel benzylidenephenylpyrrolizinones with pleiotropic activities potentially useful in Alzheimer's disease treatment.

Abstract：

:This work describes the synthesis and the biological evaluation of novel benzylidenephenylpyrrolizinones as potential antioxidant, metal chelating or amyloid β (βA) aggregation inhibitors. Some derivatives exhibited interesting results in regard to several of the performed evaluations and appear as valuable Multi-Target Directed Ligands with potential therapeutic interest in Alzheimer's disease. Among them, compound 29 particularly appears as a valuable radical and NO scavenger, a Cu(II) and Fe(II) chelating agent and exhibits moderate βA aggregation inhibition properties. These activities, associated to a good predictive bioavailability and a lack of cytotoxicity, design it as a promising hit for further in vivo investigation.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Jourdan JP,Since M,El Kihel L,Lecoutey C,Corvaisier S,Legay R,Sopkova-de Oliveira Santos J,Cresteil T,Malzert-Fréon A,Rochais C,Dallemagne P

doi

10.1016/j.ejmech.2016.03.023

subject

Has Abstract

pub_date

2016-05-23 00:00:00

pages

365-79

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(16)30197-0

journal_volume

114

pub_type

杂志文章

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