2. Academic Validation
  3. Inhibition of acetylcholinesterase, beta-amyloid aggregation, and NMDA receptors in Alzheimer's disease: a promising direction for the multi-target-directed ligands gold rush

Inhibition of acetylcholinesterase, beta-amyloid aggregation, and NMDA receptors in Alzheimer's disease: a promising direction for the multi-target-directed ligands gold rush

  • J Med Chem. 2008 Aug 14;51(15):4381-4. doi: 10.1021/jm800577j.
Michela Rosini 1,  Elena Simoni,  Manuela Bartolini,  Andrea Cavalli,  Luisa Ceccarini,  Nicoleta Pascu,  David W McClymont,  Andrea Tarozzi,  Maria L Bolognesi,  Anna Minarini,  Vincenzo Tumiatti,  Vincenza Andrisano,  Ian R Mellor,  Carlo Melchiorre
Affiliations

Affiliation

  • 1 Department of Pharmaceutical Sciences, Alma Mater Studiorum, UniVersity of Bologna, Via Belmeloro 6, I-40126 Bologna, Italy. michela.rosini@unibo.it
PMID: 18605718 DOI: 10.1021/jm800577j
Abstract

Alzheimer's disease (AD) is a multifactorial syndrome with several target proteins contributing to its etiology. To confront AD, an innovative strategy is to design single chemical entities able to simultaneously modulate more than one target. Here, we present compounds that inhibit acetylcholinesterase and NMDA Receptor activity. Furthermore, these compounds inhibit AChE-induced Abeta aggregation and display antioxidant properties, emerging as lead candidates for treating AD.

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