Fluorinated benzophenone derivatives: Balanced multipotent agents for Alzheimer's disease
Research output: Contribution to journal › Article › peer-review
Authors
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 language | English |
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Pages (from-to) | 157-166 |
Number of pages | 10 |
Journal | European Journal of Medicinal Chemistry |
Volume | 78 |
Early online date | 16 Mar 2014 |
Publication status | Published - 6 May 2014 |
Keywords
- Acetylcholinesterase, Alzheimer's disease, Antioxidant activity, BACE-1, Benzophenone, Drug design, Lead identification