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
Belluti F., De Simone A., Tarozzi A., Bartolini M., Djemil A., Bisi A., et al. (2014). Fluorinated benzophenone derivatives: balanced multipotent agents for Alzheimer's disease. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 78, 157-166 [10.1016/j.ejmech.2014.03.042].
Fluorinated benzophenone derivatives: balanced multipotent agents for Alzheimer's disease
BELLUTI, FEDERICA;DE SIMONE, ANGELA;TAROZZI, ANDREA;BARTOLINI, MANUELA;BISI, ALESSANDRA;GOBBI, SILVIA;MONTANARI, SERENA;CAVALLI, ANDREA;ANDRISANO, VINCENZA;RAMPA, ANGELA
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 candidatesI documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
