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

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

De Simone A.;
2014

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
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BACE-1; Acetylcholinesterase; Alzheimer’s disease; Antioxidant activity; Benzophenone; Drug design; Lead identification
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.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2318/1719624
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