ArticleFrontiers in neuroscience2016
ASS234, As a New Multi-Target Directed Propargylamine for Alzheimer's Disease Therapy.
Article in Frontiers in neuroscience, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 73 citations in OpenAlex.
- Dual Inhibitors of Acetylcholinesterase and Monoamine Oxidase-B for the Treatment of Alzheimer's Disease.Molecules (Basel, Switzerland) · 2025Review
- Therapeutic Options in Alzheimer's Disease: From Classic Acetylcholinesterase Inhibitors to Multi-Target Drugs with Pleiotropic Activity.Life (Basel, Switzerland) · 2024Article
- Prominent Neuroprotective Potential of Indole-2-Pharmaceuticals (Basel, Switzerland) · 2024Article
- Are Terminal Alkynes Necessary for MAO-A/MAO-B Inhibition? A New Scaffold Is Revealed.Molecules (Basel, Switzerland) · 2024Article
- Recent Advancements in the Treatment of Alzheimer's Disease: A Multitarget-directed Ligand Approach.Current medicinal chemistry · 2024Review
- Latest advances in dual inhibitors of acetylcholinesterase and monoamine oxidase B against Alzheimer's disease.Journal of enzyme inhibition and medicinal chemistry · 2023Review
- Exploration of a library of piperonylic acid-derived hydrazones possessing variable aryl functionalities as potent dual cholinesterase and monoamine oxidase inhibitors.Molecular diversity · 2023Article
- A new binuclear Ni(II) complex, an effective AHeliyon · 2023Article
- Current Pharmacotherapy and Multi-Target Approaches for Alzheimer's Disease.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Design, Synthesis and Assay of Novel Methylxanthine-Alkynylmethylamine Derivatives as Acetylcholinesterase Inhibitors.Molecules (Basel, Switzerland) · 2022Article
- Amyloidosis in Alzheimer's Disease: Pathogeny, Etiology, and Related Therapeutic Directions.Molecules (Basel, Switzerland) · 2022Review
- Design, synthesis, and evaluation of 3,7-substituted coumarin derivatives as multifunctional Alzheimer's disease agents.Journal of enzyme inhibition and medicinal chemistry · 2021Article
- Critical thinking on amyloid-beta-targeted therapy: challenges and perspectives.Science China. Life sciences · 2021Review
- Solvent-free synthesis of propargylamines: an overview.RSC advances · 2021Review
- Monoamine Oxidase Inhibitors: From Classic to New Clinical Approaches.Handbook of experimental pharmacology · 2021Review
- Parameters for Irreversible Inactivation of Monoamine Oxidase.Molecules (Basel, Switzerland) · 2020Article
- Article
- New multifunctional AChE inhibitor drug prototypes protect against Aβ-induced memory deficit.Neurological sciences : official journal of the Italian Neurological Society and of the Italian Society of Clinical Neurophysiology · 2020Article
- Combining Chalcones with Donepezil to Inhibit Both Cholinesterases and Aβ Fibril Assembly.Molecules (Basel, Switzerland) · 2019Article
- In Vitro Evaluation and Docking Studies of 5-oxo-5International journal of molecular sciences · 2019Article
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Authors and funding
9 authors at 7 institutions in 4 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
highlightsASS2324 is a hybrid compound resulting from the juxtaposition of donepezil and the propargylamine PF9601N ASS2324 is a multi-target directed propargylamine able to bind to all the AChE/BuChE and MAO A/B enzymesASS2324 shows antioxidant, neuroprotective and suitable permeability propertiesASS2324 restores the scopolamine-induced cognitive impairment to the same extent as donepezil, and is less toxicASS2324 prevents β-amyloid induced aggregation in the cortex of double transgenic miceASS2324 is the most advanced anti-Alzheimer agent for pre-clinical studies that we have identified in our laboratories The complex nature of Alzheimer's disease (AD) has prompted the design of Multi-Target-Directed Ligands (MTDL) able to bind to diverse biochemical targets involved in the progress and development of the disease. In this context, we have designed a number of MTD propargylamines (MTDP) showing antioxidant, anti-beta-amyloid, anti-inflammatory, as well as cholinesterase and monoamine oxidase (MAO) inhibition capacities. Here, we describe these properties in the MTDL ASS234, our lead-compound ready to enter in pre-clinical studies for AD, as a new multipotent, permeable cholinesterase/monoamine oxidase inhibitor, able to inhibit Aβ-aggregation, and possessing antioxidant and neuroprotective properties.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.