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Anti-amyloid therapy and cerebral blood flow changes on Magnetic Resonance Imaging: a potential longitudinal biomarker of treatment response?
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From the Department of Department of Radiology, Brain Health Imaging Institute (A.R-F, J.I, S.P, M.d, G.C.C) Weill Cornell Medicine, New York-Presbyterian Hospital, New York, New York, USA; the Department of Neurology (A.R-F), Pontificia Universidad Javeriana, Bogota, Colombia; the Department of Radiology, Division of Molecular Imaging and Therapeutics (A.R-F, J.I) Weill Cornell Medicine, New York-Presbyterian Hospital, New York, New York, USA; the Department of Neurology (D.Z, MM, L.R, A.S.N) Weill Cornell Medicine, New York-Presbyterian Hospital, New York, New York, USA.
Amyloid-targeting therapy has recently become widely available in the U.S. for the treatment of patients with symptomatic mild Alzheimer's disease (AD).
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CMAJ
January 2025
Temerty Faculty of Medicine (Tilley, Kim, Lass), University of Toronto; Departments of Medicine (Silverstein) and Neurology (Masellis), Sunnybrook Health Sciences Centre, Toronto, Ont.
In vitro and in vivo Investigations of 4-Substituted 2-Phenylquinazoline derivatives as multipotent ligands for the treatment of Alzheimer's disease.
Bioorg Chem
January 2025
Laboratory of Organic and Medicinal Chemistry, Department of Chemistry, Central University of Punjab, Bathinda, India, 151401. Electronic address:
The pathology of Alzheimer's disease (AD) is complex due to its multifactorial nature and single targeting drugs proved inefficient. A series of novel 4-N-substituted-2-phenylquinazoline derivatives was designed and synthesized as potential multi-target directed ligands (MTDLs) through dual inhibition of AChE and MAO-B enzymes along with Aβ aggregation inhibition for the treatment of AD. Two compounds in the series, VAV-8 and VAV-19 were found to be the most potent inhibitors of both AChE and MAO-B enzymes and moderate inhibitor of Aβ, with good thermodynamic stability at the binding pocket of the enzymes.
View Article and Find Full Text PDFInvestigation of Thiazolidine-2,4-Dione Derivatives as Acetylcholinesterase Inhibitors: Synthesis, In Vitro Biological Activities and In Silico Studies.
ChemistryOpen
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Department of Chemistry, Faculty of Sciences, University of Guilan, Rasht, 4193833697, Iran.
The inhibition of acetylcholinesterase (AChE), an enzyme responsible for the inactivation and decrease in acetylcholine in the cholinergic pathway, has been considered an attractive target for small-molecule drug discovery in Alzheimer's disease (AD) therapy. In the present study, a series of TZD derivatives were designed, synthesized, and studied for drug likeness, blood-brain barrier (BBB) permeability, and adsorption, distribution, metabolism, excretion, and toxicity (ADMET). Additionally, docking studies of the designed compounds were performed on AChE.
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Sensors (Basel)
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Department of Mechanical Engineering and Automation, Northeastern University, Wenhua Street, Shenyang 110819, China.
The early prediction of Alzheimer's disease (AD) risk in healthy individuals remains a significant challenge. This study investigates the feasibility of task-state EEG signals for improving detection accuracy. Electroencephalogram (EEG) data were collected from the Multi-Source Interference Task (MSIT) and Sternberg Memory Task (STMT).
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