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Fluorinated benzophenone derivatives: balanced multipotent agents for Alzheimer's disease.

Abstract：

:In an effort to develop multipotent agents against β-secretase (BACE-1) and acetylcholinesterase (AChE), able to counteract intracellular ROS formation as well, the structure of the fluorinated benzophenone 3 served as starting point for the synthesis of a small library of 3-fluoro-4-hydroxy- analogues. Among the series, derivatives 5 and 12, carrying chemically different amino functions, showed a balanced micromolar potency against the selected targets. In particular, compound 12, completely devoid of toxic effects, seems to be a promising lead for obtaining effective anti-AD drug candidates.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Belluti F,De Simone A,Tarozzi A,Bartolini M,Djemil A,Bisi A,Gobbi S,Montanari S,Cavalli A,Andrisano V,Bottegoni G,Rampa A

doi

10.1016/j.ejmech.2014.03.042

subject

Has Abstract

pub_date

2014-05-06 00:00:00

pages

157-66

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(14)00255-4

journal_volume

78

pub_type

杂志文章

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