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Synthesis of Monomeric Derivatives To Probe Memoquin’s Bivalent Interactions

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journal contribution
posted on 22.12.2011, 00:00 by Maria Laura Bolognesi, GianPaolo Chiriano, Manuela Bartolini, Francesca Mancini, Giovanni Bottegoni, Valentina Maestri, Stefan Czvitkovich, Manfred Windisch, Andrea Cavalli, Anna Minarini, Michela Rosini, Vincenzo Tumiatti, Vincenza Andrisano, Carlo Melchiorre
Eight monomeric congeners, related to the multitarget lead candidate memoquin, were prepared and evaluated at multiple targets to determine their profile against Alzheimer’s disease. 24 bind to AChE with similar low nanomolar affinities and function as effective inhibitors of amyloid aggregation. The most potent monovalent ligand 2 also inhibits BACE-1 in vitro and APP metabolism in primary chicken telencephalic neurons.