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

Research output: Contribution to journalArticlepeer-review

Authors

  • Federica Belluti
  • Angela De Simone
  • Andrea Tarozzi
  • Manuela Bartolini
  • Alice Djemil
  • Alessandra Bisi
  • Silvia Gobbi
  • Serena Montanari
  • Andrea Cavalli
  • Vincenza Andrisano
  • Angela Rampa

Colleges, School and Institutes

External organisations

  • Università di Bologna
  • Istituto Italiano di Tecnologia

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.

Details

Original languageEnglish
Pages (from-to)157-166
Number of pages10
JournalEuropean Journal of Medicinal Chemistry
Volume78
Early online date16 Mar 2014
Publication statusPublished - 6 May 2014

Keywords

  • Acetylcholinesterase, Alzheimer's disease, Antioxidant activity, BACE-1, Benzophenone, Drug design, Lead identification