Cargando…

Synthesis, Molecular Modelling and Biological Evaluation of Novel Heterodimeric, Multiple Ligands Targeting Cholinesterases and Amyloid Beta

Cholinesterases and amyloid beta are one of the major biological targets in the search for a new and efficacious treatment of Alzheimer’s disease. The study describes synthesis and pharmacological evaluation of new compounds designed as dual binding site acetylcholinesterase inhibitors. Among the sy...

Descripción completa

Detalles Bibliográficos
Autores principales:	Hebda, Michalina, Bajda, Marek, Więckowska, Anna, Szałaj, Natalia, Pasieka, Anna, Panek, Dawid, Godyń, Justyna, Wichur, Tomasz, Knez, Damijan, Gobec, Stanislav, Malawska, Barbara
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	MDPI 2016
Materias:	Article
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273065/ https://www.ncbi.nlm.nih.gov/pubmed/27023510 http://dx.doi.org/10.3390/molecules21040410

Ejemplares similares

Design, Synthesis, and Biological Evaluation of 2-(Benzylamino-2-Hydroxyalkyl)Isoindoline-1,3-Diones Derivatives as Potential Disease-Modifying Multifunctional Anti-Alzheimer Agents
por: Panek, Dawid, et al.
Publicado: (2018)

Multidirectional in vitro and in cellulo studies as a tool for identification of multi-target-directed ligands aiming at symptoms and causes of Alzheimer’s disease
por: Szałaj, Natalia, et al.
Publicado: (2020)

Dual Inhibitors of Amyloid-β and Tau Aggregation with Amyloid-β Disaggregating Properties: Extended In Cellulo, In Silico, and Kinetic Studies of Multifunctional Anti-Alzheimer’s Agents
por: Pasieka, Anna, et al.
Publicado: (2021)

Structure-Based Search for New Inhibitors of Cholinesterases
por: Bajda, Marek, et al.
Publicado: (2013)

Guanidines: Synthesis of Novel Histamine H(3)R Antagonists with Additional Breast Anticancer Activity and Cholinesterases Inhibitory Effect
por: Staszewski, Marek, et al.
Publicado: (2023)

Synthesis and Biological Evaluation of Benzochromenopyrimidinones as Cholinesterase Inhibitors and Potent Antioxidant, Non-Hepatotoxic Agents for Alzheimer’s Disease
por: Dgachi, Youssef, et al.
Publicado: (2016)

Serotonin 5-HT(6) Receptor Ligands and Butyrylcholinesterase Inhibitors Displaying Antioxidant Activity—Design, Synthesis and Biological Evaluation of Multifunctional Agents against Alzheimer’s Disease
por: Więckowski, Krzysztof, et al.
Publicado: (2022)

Benzophenone Derivatives with Histamine H(3) Receptor Affinity and Cholinesterase Inhibitory Potency as Multitarget-Directed Ligands for Possible Therapy of Alzheimer’s Disease
por: Godyń, Justyna, et al.
Publicado: (2022)

N-Hydroxy-N-Propargylamide Derivatives of Ferulic Acid: Inhibitors of Cholinesterases and Monoamine Oxidases
por: Bautista-Aguilera, Óscar M., et al.
Publicado: (2022)

Dual Action of Dipyridothiazine and Quinobenzothiazine Derivatives—Anticancer and Cholinesterase-Inhibiting Activity
por: Jończyk, Jakub, et al.
Publicado: (2020)

Screening of Big Pharma’s Library against Various in-house Biological Targets
por: Knez, Damijan, et al.
Publicado: (2022)

Biological Evaluation of Valeriana Extracts from Argentina with Potent Cholinesterase Inhibition for the Treatment of Neurodegenerative Disorders and Their Comorbidities—The Case of Valeriana carnosa Sm. (Caprifoliaceae) Studied in Mice
por: Marcucci, Carolina, et al.
Publicado: (2023)

4-Phenethyl-1-Propargylpiperidine-Derived Dual Inhibitors of Butyrylcholinesterase and Monoamine Oxidase B
por: Mazej, Tjaša, et al.
Publicado: (2021)

Biphenylalkoxyamine Derivatives–Histamine H(3) Receptor Ligands with Butyrylcholinesterase Inhibitory Activity
por: Łażewska, Dorota, et al.
Publicado: (2021)

Recent Development of Multifunctional Agents as Potential Drug Candidates for the Treatment of Alzheimer's Disease
por: Guzior, Natalia, et al.
Publicado: (2015)

Development of an in-vivo active reversible butyrylcholinesterase inhibitor
por: Košak, Urban, et al.
Publicado: (2016)

Multitargeting Histamine H(3) Receptor Ligands among Acetyl- and Propionyl-Phenoxyalkyl Derivatives
por: Łażewska, Dorota, et al.
Publicado: (2023)

Fragment-Sized Thiazoles in Fragment-Based Drug Discovery Campaigns: Friend or Foe?
por: Proj, Matic, et al.
Publicado: (2022)

Synthesis and Initial Characterization of a Reversible, Selective (18)F-Labeled Radiotracer for Human Butyrylcholinesterase
por: Gentzsch, Christian, et al.
Publicado: (2021)

WIDOCK: a reactive docking protocol for virtual screening of covalent inhibitors
por: Scarpino, Andrea, et al.
Publicado: (2021)

Hybrid approach to structure modeling of the histamine H3 receptor: Multi-level assessment as a tool for model verification
por: Jończyk, Jakub, et al.
Publicado: (2017)

Can Activation of Acetylcholinesterase by β-Amyloid Peptide Decrease the Effectiveness of Cholinesterase Inhibitors?
por: Zueva, Irina V., et al.
Publicado: (2023)

SAT271 Ligand Induced GR Heterodimerization With MR In Living Cells
por: Sueyoshi, Tatsuya, et al.
Publicado: (2023)

Evaluation of novel cathepsin-X inhibitors in vitro and in vivo and their ability to improve cathepsin-B-directed antitumor therapy
por: Mitrović, Ana, et al.
Publicado: (2022)

8-Hydroxyquinolylnitrones as multifunctional ligands for the therapy of neurodegenerative diseases
por: Knez, Damijan, et al.
Publicado: (2023)

Development of potent reversible selective inhibitors of butyrylcholinesterase as fluorescent probes
por: Pajk, Stane, et al.
Publicado: (2020)

Application of Computational Methods for the Design of BACE-1 Inhibitors: Validation of in Silico Modelling
por: Bajda, Marek, et al.
Publicado: (2014)

Ligand Dependent Switch from RXR Homo- to RXR-NURR1 Heterodimerization
por: Scheepstra, Marcel, et al.
Publicado: (2017)

Fragment-Sized and Bidentate (Immuno)Proteasome Inhibitors Derived from Cysteine and Threonine Targeting Warheads
por: Kollár, Levente, et al.
Publicado: (2021)

Polyfunctionalized α-Phenyl-tert-butyl(benzyl)nitrones: Multifunctional Antioxidants for Stroke Treatment
por: Diez-Iriepa, Daniel, et al.
Publicado: (2022)

Identification and characterization of the novel reversible and selective cathepsin X inhibitors
por: Fonović, Urša Pečar, et al.
Publicado: (2017)

Next-Generation Heterocyclic Electrophiles as Small-Molecule Covalent MurA Inhibitors
por: Ábrányi-Balogh, Péter, et al.
Publicado: (2022)

Neuroactive Multifunctional Tacrine Congeners with Cholinesterase, Anti-Amyloid Aggregation and Neuroprotective Properties
por: Kozurkova, Maria, et al.
Publicado: (2011)

Potential of Vitamin B6 Dioxime Analogues to Act as Cholinesterase Ligands
por: Gašo Sokač, Dajana, et al.
Publicado: (2022)

Discovery of Novel Small-Molecule Compounds with Selective Cytotoxicity for Burkitt’s Lymphoma Cells Using 3D Ligand-Based Virtual Screening
por: Gobec, Martina, et al.
Publicado: (2014)

Protein Dynamics of the HIF-2α PAS-B Domain upon Heterodimerization and Ligand Binding
por: Masetti, Matteo, et al.
Publicado: (2014)

Ligand-Regulated Heterodimerization of Peroxisome Proliferator-Activated Receptor α with Liver X Receptor α
por: Balanarasimha, Madhumitha, et al.
Publicado: (2014)

Heterodimeric Plasmonic Nanogaps for Biosensing
por: Chatterjee, Sharmistha, et al.
Publicado: (2018)

Hydroxybenzoic Acid Derivatives as Dual-Target Ligands: Mitochondriotropic Antioxidants and Cholinesterase Inhibitors
por: Oliveira, Catarina, et al.
Publicado: (2018)

Forced Homo- and Heterodimerization of All gp130-Type Receptor Complexes Leads to Constitutive Ligand-independent Signaling and Cytokine-independent Growth
por: Suthaus, Jan, et al.
Publicado: (2010)

Cannot write session to /tmp/vufind_sessions/sess_j1a9quj3tvfeu4udulb12vh1l5