Structure− activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer

V Tumiatti, A Milelli, A Minarini, M Rosini…

Index: Tumiatti, Vincenzo; Milelli, Andrea; Minarini, Anna; Rosini, Michela; Bolognesi, Maria Laura; Micco, Marialuisa; Andrisano, Vincenza; Bartolini, Manuela; Mancini, Francesca; Recanatini, Maurizio; Cavalli, Andrea; Melchiorre, Carlo Journal of Medicinal Chemistry, 2008 , vol. 51, # 22 p. 7308 - 7312

Full Text: HTML

Citation Number: 53

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 β-amyloid aggregation in the micromolar range.