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The Bivalent Ligand Approach as a Tool for Improving the in vitro Anti‐Alzheimer Multitarget Profile of Dimebon
Author(s) -
Rosini Michela,
Simoni Elena,
Bartolini Manuela,
Soriano Elena,
MarcoContelles José,
Andrisano Vincenza,
Monti Barbara,
Windisch Manfred,
HutterPaier Birgit,
McClymont David W.,
Mellor Ian R.,
Bolognesi Maria Laura
Publication year - 2013
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201300263
Subject(s) - bivalent (engine) , in vitro , chemistry , computational biology , computer science , neuroscience , combinatorial chemistry , biochemistry , biology , organic chemistry , metal
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, Aβ 42 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.