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American Chemical Society, Journal of Medicinal Chemistry, 24(54), p. 8299-8304, 2011

DOI: 10.1021/jm200691d

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Synthesis of monomeric derivatives to probe memoquin's bivalent interactions

Journal article published in 2011 by Maria Laura Bolognesi, GianPaolo Chiriano, Manuela Bartolini ORCID, Francesca Mancini, Giovanni Bottegoni, Valentina Maestri, Stefan Czvitkovich, Manfred Windisch, Andrea Cavalli, Anna Minarini, Michela Rosini, Vincenzo Tumiatti, Vincenza Andrisano, Carlo Melchiorre
This paper was not found in any repository; the policy of its publisher is unknown or unclear.
This paper was not found in any repository; the policy of its publisher is unknown or unclear.

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Abstract

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. 2-4 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.