Inspired by the concept of bivalent ligands, we prepared a small set of analogues of the drug candidate dimebon. They were shown to inhibit AChE, Aβ42 aggregation, and NMDA receptor activation to a greater extent than dimebon. Some of these compounds also enhanced the survival of chicken neurons under apoptosis-inducing conditions.
The bivalent ligand approach as a tool for improving the in vitro anti-Alzheimer multitarget profile of dimebon / Michela Rosini; Elena Simoni; Manuela Bartolini; Elena Soriano; José Marco-Contelles; Vincenza Andrisano; Barbara Monti; Manfred Windisch; Birgit Hutter-Paier; David W. McClymont; Ian R. Mellor; Maria Laura Bolognesi. - In: CHEMMEDCHEM. - ISSN 1860-7179. - STAMPA. - 8:(2013), pp. 1276-1281. [10.1002/cmdc.201300263]
The bivalent ligand approach as a tool for improving the in vitro anti-Alzheimer multitarget profile of dimebon
ROSINI, MICHELA;SIMONI, ELENA;BARTOLINI, MANUELA;ANDRISANO, VINCENZA;MONTI, BARBARA;BOLOGNESI, MARIA LAURA
2013
Abstract
Inspired by the concept of bivalent ligands, we prepared a small set of analogues of the drug candidate dimebon. They were shown to inhibit AChE, Aβ42 aggregation, and NMDA receptor activation to a greater extent than dimebon. Some of these compounds also enhanced the survival of chicken neurons under apoptosis-inducing conditions.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
