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American Chemical Society, Journal of Medicinal Chemistry, 22(51), p. 7308-7312, 2008

DOI: 10.1021/jm8009684

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Structure-Activity Relationships of Acetylcholinesterase Noncovalent Inhibitors Based on a Polyamine Backbone. 4. Further Investigation on the Inner Spacer

Journal article published in 2008 by Vincenzo Tumiatti, Andrea Milelli, Anna Minarini, Michela Rosini, Maria Laura Bolognesi, Marialuisa Micco, Vincenza Andrisano, Manuela Bartolini ORCID, Francesca Mancini, Maurizio Recanatini, Andrea Cavalli, Carlo Melchiorre
This paper is available in a repository.
This paper is available in a repository.

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Abstract

Novel multi-target-directed ligands were designed by replacing the inner dipiperidino function of 3 with less flexible or completely rigid moieties to obtain compounds endowed with multiple biological properties that might be relevant to Alzheimer's disease. 15 was the most interesting, inhibiting AChE in the nanomolar range and inhibiting AChE-induced and self-promoted beta-amyloid aggregation in the micromolar range.