Literature DB >> 18605718

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

Michela Rosini1, 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.   

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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Year:  2008        PMID: 18605718     DOI: 10.1021/jm800577j

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  27 in total

1.  Design, synthesis and structure-activity relationship (SAR) studies of 2,4-disubstituted pyrimidine derivatives: dual activity as cholinesterase and Aβ-aggregation inhibitors.

Authors:  Tarek Mohamed; Xiaobei Zhao; Lila K Habib; Jerry Yang; Praveen P N Rao
Journal:  Bioorg Med Chem       Date:  2011-03-01       Impact factor: 3.641

2.  Synthesis and functional survey of new Tacrine analogs modified with nitroxides or their precursors.

Authors:  Tamás Kálai; Robin Altman; Izumi Maezawa; Mária Balog; Christophe Morisseau; Jitka Petrlova; Bruce D Hammock; Lee-Way Jin; James R Trudell; John C Voss; Kálmán Hideg
Journal:  Eur J Med Chem       Date:  2014-03-12       Impact factor: 6.514

3.  Molecular docking and receptor-specific 3D-QSAR studies of acetylcholinesterase inhibitors.

Authors:  Pran Kishore Deb; Anuradha Sharma; Poonam Piplani; Raghuram Rao Akkinepally
Journal:  Mol Divers       Date:  2012-09-21       Impact factor: 2.943

Review 4.  Multi-target design strategies in the context of Alzheimer's disease: acetylcholinesterase inhibition and NMDA receptor antagonism as the driving forces.

Authors:  Michela Rosini; Elena Simoni; Anna Minarini; Carlo Melchiorre
Journal:  Neurochem Res       Date:  2014-02-04       Impact factor: 3.996

Review 5.  Rational approaches, design strategies, structure activity relationship and mechanistic insights for therapeutic coumarin hybrids.

Authors:  Harbinder Singh; Jatinder Vir Singh; Kavita Bhagat; Harmandeep Kaur Gulati; Mohit Sanduja; Nitish Kumar; Nihar Kinarivala; Sahil Sharma
Journal:  Bioorg Med Chem       Date:  2019-06-22       Impact factor: 3.641

Review 6.  Multi-Target Drug Candidates for Multifactorial Alzheimer's Disease: AChE and NMDAR as Molecular Targets.

Authors:  Md Sahab Uddin; Abdullah Al Mamun; Md Tanvir Kabir; Ghulam Md Ashraf; May N Bin-Jumah; Mohamed M Abdel-Daim
Journal:  Mol Neurobiol       Date:  2020-09-15       Impact factor: 5.590

7.  sym-Triazines for directed multitarget modulation of cholinesterases and amyloid-β in Alzheimer's disease.

Authors:  Anthony J Veloso; Devjani Dhar; Ari M Chow; Biao Zhang; Derek W F Tang; Hashwin V S Ganesh; Svetlana Mikhaylichenko; Ian R Brown; Kagan Kerman
Journal:  ACS Chem Neurosci       Date:  2012-11-20       Impact factor: 4.418

Review 8.  Hybrids: a new paradigm to treat Alzheimer's disease.

Authors:  Manjinder Singh; Maninder Kaur; Navriti Chadha; Om Silakari
Journal:  Mol Divers       Date:  2015-09-02       Impact factor: 2.943

9.  Ethanol preconditioning of rat cerebellar cultures targets NMDA receptors to the synapse and enhances peroxiredoxin 2 expression.

Authors:  Robert M Mitchell; Nuzhath Tajuddin; Edward M Campbell; Edward J Neafsey; Michael A Collins
Journal:  Brain Res       Date:  2016-03-25       Impact factor: 3.252

Review 10.  Stabilizers of neuronal and mitochondrial calcium cycling as a strategy for developing a medicine for Alzheimer's disease.

Authors:  José-Carlos Fernández-Morales; Juan-Alberto Arranz-Tagarro; Enrique Calvo-Gallardo; Marcos Maroto; Juan-Fernando Padín; Antonio G García
Journal:  ACS Chem Neurosci       Date:  2012-08-29       Impact factor: 4.418

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