Synthesis of monomeric derivatives to probe memoquin's bivalent interactions

Maria Laura Bolognesi*, Gian Paolo 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

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

27 Citations (Scopus)


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. (Figure presented)

Original languageEnglish
Pages (from-to)8299-8304
Number of pages6
JournalJournal of Medicinal Chemistry
Issue number24
Publication statusPublished - 22 Dec 2011
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery


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