Search Results - "Godyń, Justyna"
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Therapeutic strategies for Alzheimer's disease in clinical trials
Published in Pharmacological reports (01-02-2016)“…Alzheimer's disease (AD) is considered to be the most common cause of dementia and is an incurable, progressive neurodegenerative disorder. Current treatment…”
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Design, synthesis and biological evaluation of new phthalimide and saccharin derivatives with alicyclic amines targeting cholinesterases, beta-secretase and amyloid beta aggregation
Published in European journal of medicinal chemistry (05-01-2017)“…The complexity of Alzheimer's disease (AD) calls for search of multifunctional compounds as potential candidates for effective therapy. A series of phthalimide…”
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Dual Action of Dipyridothiazine and Quinobenzothiazine Derivatives-Anticancer and Cholinesterase-Inhibiting Activity
Published in Molecules (Basel, Switzerland) (03-06-2020)“…The inverse correlation observed between Alzheimer's disease (AD) and cancer has prompted us to look for cholinesterase-inhibiting activity in phenothiazine…”
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1-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer’s disease
Published in European journal of medicinal chemistry (01-02-2020)“…Complex pathomechanism of Alzheimer’s disease (AD) prompts researchers to develop multifunctional molecules in order to find effective therapy against AD. We…”
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Search for new multi-target compounds against Alzheimer's disease among histamine H 3 receptor ligands
Published in European journal of medicinal chemistry (01-01-2020)“…Multi-target-directed ligands seem to be an interesting approach to the treatment of complex disorders such as Alzheimer's disease. The aim of the present…”
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Design, Synthesis, and Biological Evaluation of 1‑Benzylamino-2-hydroxyalkyl Derivatives as New Potential Disease-Modifying Multifunctional Anti-Alzheimer’s Agents
Published in ACS chemical neuroscience (16-05-2018)“…The multitarget approach is a promising paradigm in drug discovery, potentially leading to new treatment options for complex disorders, such as Alzheimer’s…”
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Multifunctional agents against Alzheimer's disease based on oxidative stress: Polysubstituted pyrazine derivatives synthesized by multicomponent reactions
Published in Bioorganic & medicinal chemistry (15-12-2023)“…As Alzheimer's disease (AD) is a neurodegenerative disease with a complex pathogenesis, the exploration of multi-target drugs may be an effective strategy for…”
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Design, Synthesis, and Biological Evaluation of 2-(Benzylamino-2-Hydroxyalkyl)Isoindoline-1,3-Diones Derivatives as Potential Disease-Modifying Multifunctional Anti-Alzheimer Agents
Published in Molecules (Basel, Switzerland) (07-02-2018)“…The complex nature of Alzheimer's disease calls for multidirectional treatment. Consequently, the search for multi-target-directed ligands may lead to…”
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New Dual Small Molecules for Alzheimer’s Disease Therapy Combining Histamine H3 Receptor (H3R) Antagonism and Calcium Channels Blockade with Additional Cholinesterase Inhibition
Published in Journal of medicinal chemistry (26-12-2019)“…New tritarget small molecules combining Ca2+ channels blockade, cholinesterase, and H3 receptor inhibition were obtained by multicomponent synthesis. Compound…”
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4‑Oxypiperidine Ethers as Multiple Targeting Ligands at Histamine H3 Receptors and Cholinesterases
Published in ACS chemical neuroscience (20-03-2024)“…This study examines the properties of a novel series of 4-oxypiperidines designed and synthesized as histamine H3R antagonists/inverse agonists based on the…”
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Discovery of New Highly Potent Histamine H3 Receptor Antagonists, Calcium Channel Blockers, and Acetylcholinesterase Inhibitors
Published in ACS chemical neuroscience (18-09-2024)“…At present, one of the most promising strategies to tackle the complex challenges posed by Alzheimer’s disease (AD) involves the development of novel…”
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Exploring Novel GSK-3β Inhibitors for Anti-Neuroinflammatory and Neuroprotective Effects: Synthesis, Crystallography, Computational Analysis, and Biological Evaluation
Published in ACS chemical neuroscience (04-09-2024)“…In the pathogenesis of Alzheimer’s disease, the overexpression of glycogen synthase kinase-3β (GSK-3β) stands out due to its multifaced nature, as it…”
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Novel Multitarget-Directed Ligands Aiming at Symptoms and Causes of Alzheimer’s Disease
Published in ACS chemical neuroscience (16-05-2018)“…Alzheimer’s disease (AD) is a major public health problem, which is due to its increasing prevalence and lack of effective therapy or diagnostics. The…”
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Discovery of new, highly potent and selective inhibitors of BuChE - design, synthesis, in vitro and in vivo evaluation and crystallography studies
Published in European journal of medicinal chemistry (05-03-2023)“…The symptomatic and disease-modifying effects of butyrylcholinesterase (BuChE) inhibitors provide an encouraging premise for researching effective treatments…”
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Discovery of 1-(phenylsulfonyl)-1H-indole-based multifunctional ligands targeting cholinesterases and 5-HT6 receptor with anti-aggregation properties against amyloid-beta and tau
Published in European journal of medicinal chemistry (05-12-2021)“…Multifunctional ligands as an essential variant of polypharmacology are promising candidates for the treatment of multi-factorial diseases like Alzheimer's…”
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Contilisant+Tubastatin A Hybrids: Polyfunctionalized Indole Derivatives as New HDAC Inhibitor-Based Multitarget Small Molecules with In Vitro and In Vivo Activity in Neurodegenerative Diseases
Published in Journal of medicinal chemistry (26-09-2024)“…Herein, we describe the design, synthesis, and biological evaluation of 15 Contilisant+Tubastatin A hybrids. These ligands are polyfunctionalized indole…”
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Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy
Published in European journal of medicinal chemistry (27-01-2017)“…Herein we report an efficient two step synthesis and biological assessment of 12 racemic tetrahydropyranodiquinolin-8-amines derivatives as antioxidant,…”
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Benzophenone Derivatives with Histamine H3 Receptor Affinity and Cholinesterase Inhibitory Potency as Multitarget-Directed Ligands for Possible Therapy of Alzheimer’s Disease
Published in Molecules (Basel, Switzerland) (28-12-2022)“…The multitarget-directed ligands demonstrating affinity to histamine H3 receptor and additional cholinesterase inhibitory potency represent a promising…”
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Biphenylalkoxyamine Derivatives–Histamine H3 Receptor Ligands with Butyrylcholinesterase Inhibitory Activity
Published in Molecules (Basel, Switzerland) (11-06-2021)“…Neurodegenerative diseases, e.g., Alzheimer’s disease (AD), are a key health problem in the aging population. The lack of effective therapy and diagnostics…”
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Anti‐Alzheimer's multitarget‐directed ligands with serotonin 5‐HT6 antagonist, butyrylcholinesterase inhibitory, and antioxidant activity
Published in Archiv der Pharmazie (Weinheim) (01-07-2019)“…Serotonin 5‐HT6 receptors, butyrylcholinesterase (BuChE) and oxidative stress are related to the pathophysiology of Alzheimer's disease. Inhibition of BuChE…”
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