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

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

doi:10.1016/j.ejmech.2014.03.042

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

Federica Belluti^*, Angela De Simone, Andrea Tarozzi, Manuela Bartolini, Alice Djemil, Alessandra Bisi, Silvia Gobbi, Serena Montanari, Andrea Cavalli, Vincenza Andrisano, Giovanni Bottegoni, Angela Rampa

^*Corresponding author for this work

Pharmacy

Research output: Contribution to journal › Article › peer-review

21 Citations (Scopus)

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.

Original language	English
Pages (from-to)	157-166
Number of pages	10
Journal	European Journal of Medicinal Chemistry
Volume	78
Early online date	16 Mar 2014
DOIs	https://doi.org/10.1016/j.ejmech.2014.03.042
Publication status	Published - 6 May 2014

Keywords

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

ASJC Scopus subject areas

Pharmacology
Drug Discovery
Organic Chemistry

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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. (2014). Fluorinated benzophenone derivatives: Balanced multipotent agents for Alzheimer's disease. European Journal of Medicinal Chemistry, 78, 157-166. Advance online publication. https://doi.org/10.1016/j.ejmech.2014.03.042

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title = "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.",

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

author = "Federica Belluti and {De Simone}, Angela and Andrea Tarozzi and Manuela Bartolini and Alice Djemil and Alessandra Bisi and Silvia Gobbi and Serena Montanari and Andrea Cavalli and Vincenza Andrisano and Giovanni Bottegoni and Angela Rampa",

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T1 - Fluorinated benzophenone derivatives

T2 - Balanced multipotent agents for Alzheimer's disease

AU - Belluti, Federica

AU - De Simone, Angela

AU - Tarozzi, Andrea

AU - Bartolini, Manuela

AU - Djemil, Alice

AU - Bisi, Alessandra

AU - Gobbi, Silvia

AU - Montanari, Serena

AU - Cavalli, Andrea

AU - Andrisano, Vincenza

AU - Bottegoni, Giovanni

AU - Rampa, Angela

PY - 2014/5/6

Y1 - 2014/5/6

N2 - 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.

AB - 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.

KW - Acetylcholinesterase

KW - Alzheimer's disease

KW - Antioxidant activity

KW - BACE-1

KW - Benzophenone

KW - Drug design

KW - Lead identification

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M3 - Article

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AN - SCOPUS:84897444798

SN - 0223-5234

VL - 78

SP - 157

EP - 166

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

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

Abstract

Keywords

ASJC Scopus subject areas

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