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.
V. Tumiatti, A. Milelli, A. Minarini, M. Rosini, M. L. Bolognesi, M. Micco, et al. (2008). Structure-Activity Relationships of Acetylcholinesterase Noncovalent Inhibitors Based on a Polyamine Backbone. 4. Futher Investigation on the Inner Spacer. JOURNAL OF MEDICINAL CHEMISTRY, 51, 7308-7312 [10.1021/jm8009684].
Structure-Activity Relationships of Acetylcholinesterase Noncovalent Inhibitors Based on a Polyamine Backbone. 4. Futher Investigation on the Inner Spacer.
TUMIATTI, VINCENZO;MILELLI, ANDREA;MINARINI, ANNA;ROSINI, MICHELA;BOLOGNESI, MARIA LAURA;ANDRISANO, VINCENZA;BARTOLINI, MANUELA;MANCINI, FRANCESCO;RECANATINI, MAURIZIO;CAVALLI, ANDREA;MELCHIORRE, CARLO
2008
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
