Inhibition of Acetylcholinesterase, β-Amyloid Aggregation, and NMDA Receptors in Alzheimer’s Disease: A Promising Direction for the Multi-target-Directed Ligands Gold Rush

Michela Rosini*†, Elena Simoni†, Manuela Bartolini†, Andrea Cavalli†, Luisa Ceccarini†, Nicoleta Pascu‡, David W. McClymont‡, Andrea Tarozzi§, Maria L. Bolognesi†, Anna Minarini†, Vincenzo Tumiatti†, Vincenza Andrisano†, Ian R. Mellor‡ and Carlo Melchiorre*†
Departments of Pharmaceutical Sciences and Pharmacology, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, I-40126 Bologna, Italy, and School of Biology, University of Nottingham, University Park Nottingham NG7 2RD U.K.
J. Med. Chem., 2008, 51 (15), pp 4381–4384
DOI: 10.1021/jm800577j
Publication Date (Web): July 8, 2008
Copyright © 2008 American Chemical Society
* To whom correspondence should be addressed. Telephone: +390512099700. Fax: +390512099734. E-mail: for M.R., michela.rosini@unibo.it; for C.M., carlo.melchiorre@unibo.it.
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†

Department of Pharmaceutical Sciences, University of Bologna.

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‡

University of Nottingham.

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§

Department of Pharmacology, University of Bologna.

Abstract

Abstract Image

Alzheimer’s disease (AD) is a multifactorial syndrome with several target proteins contributing to its etiology. To confront AD, an innovative strategy is to design single chemical entities able to simultaneously modulate more than one target. Here, we present compounds that inhibit acetylcholinesterase and NMDA receptor activity. Furthermore, these compounds inhibit AChE-induced Aβ aggregation and display antioxidant properties, emerging as lead candidates for treating AD.

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History

  • Published In Issue August 14, 2008
  • Article ASAPJuly 08, 2008
  • Received: May 16, 2008

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