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Polycyclic maleimide-based derivatives as first dual modulators of neuronal calcium channels and GSK-3β for Alzheimer's disease treatment.

Abstract：

:Current healthcare has significantly increased the average life expectancy, leading to a consequently greater incidence of age-related diseases, such as Alzheimer's disease. Following a multitarget approach, in this paper a series of polycyclic maleimide-based derivatives were designed and synthesized aimed at simultaneously modulate neuronal calcium channels and glycogen synthase kinase 3-beta (GSK-3β), validated targets to combat Alzheimer' disease. Different structural modifications were performed on the polycyclic scaffold in order to investigate the structure-activity relationships and compound 10 emerged as a promising non-toxic lead compound, endowed with calcium modulating brain-addressed properties and significant GSK-3β inhibitory activity. Moreover, the easily affordable polycyclic core appears as a new appealing privileged structure in medicinal chemistry.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Bisi A,Arribas RL,Micucci M,Budriesi R,Feoli A,Castellano S,Belluti F,Gobbi S,de Los Rios C,Rampa A

doi

10.1016/j.ejmech.2018.12.003

subject

Has Abstract

pub_date

2019-02-01 00:00:00

pages

394-402

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(18)31040-7

journal_volume

163

pub_type

杂志文章

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