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- || Cognex (tacrine) / Shionogi
Review, Journal: Innovative Therapeutic Strategies in Alzheimer's Disease: A Synergistic Approach to Neurodegenerative Disorders. (Pubmed Central) - Jun 27, 2024
This necessity has led to the incorporation advanced technologies like artificial intelligence and machine learning into the drug discovery process for neurodegenerative diseases. These technologies help identify therapeutic targets and optimize lead compounds, offering a more effective approach to addressing the challenges of AD and similar conditions.
- | Cognex (tacrine) / Shionogi
Journal: Pro-cognitive effects of dual tacrine derivatives acting as cholinesterase inhibitors and NMDA receptor antagonists. (Pubmed Central) - Jun 19, 2024
We conclude that tacrine has the potential for development of derivatives with dual in vivo effects. Our findings contributed to the elucidation of the structural and functional properties of tacrine derivatives associated with optimal in vivo pro-cognitive efficacy.
- | Cognex (tacrine) / Shionogi
Journal: Computational Investigation of Novel Compounds as Dual Inhibitors of AChE and GSK-3? for the Treatment of Alzheimer's Disease. (Pubmed Central) - Jun 11, 2024
and AChE simultaneously. So, in the future, the designing and development of dual inhibitors will harbinger a new era of drug design in AD treatment.
- | Cognex (tacrine) / Shionogi
Journal: A computational approach to identify phytochemicals as potential inhibitor of acetylcholinesterase: Molecular docking, ADME profiling and molecular dynamics simulations. (Pubmed Central) - Jun 4, 2024
The investigation suggested 3 ligands as a potent inhibitor of AChE which are [3-(1-methylpiperidin-2-yl)phenyl] N,N-diethylcarbamate, 4-Amino-2-styrylquinoline and bisdemethoxycurcumin. Furthermore, investigation, including in-vitro and in-vivo studies, is needed to validate the efficacy, safety profiles, and therapeutic potential of these compounds for AD treatment.
- | Cognex (tacrine) / Shionogi
Journal: Computational identification of potential acetylcholinesterase (AChE) and monoamine oxidase-B inhibitors from Vitis vinifera: a case study of Alzheimer's disease (AD). (Pubmed Central) - Jun 3, 2024
A number of Vitis vinifera-derived bioactive compounds show excellent inhibitory potential against AChE and MAO-B, and moderate pharmacokinetic features when compared to the reference ligand (tacrine). These compounds are therefore proposed as novel AChE and MAO-B inhibitors for the treatment of AD and wet-lab analysis is necessary to affirm their potency.
- | Cognex (tacrine) / Shionogi
Journal: Novel diarylated tacrine derivatives: Synthesis, characterization, anticancer, antiepileptic, antibacterial, and antifungal activities. (Pubmed Central) - Apr 13, 2024
The results suggest their potential for further exploration as cancer-specific, enzyme inhibitory, and antibacterial therapeutic agents. Notably, four compounds, namely, 5,7-bis(4-(methylthio)phenyl)tacrine (3d), 5,7-bis(4-(trifluoromethoxy)phenyl)tacrine (3e), 2,4-bis(4-(trifluoromethoxy)phenyl)-7,8,9,10-tetrahydro-6H-cyclohepta[b]quinolin-11-amine (4e), and 6,8-dibromotacrine (3), emerged as the most promising candidates for preclinical studies.
- | Cognex (tacrine) / Shionogi
Journal: Disentangling the formation, mechanism, and evolvement of the covalent methanesulfonyl fluoride acetylcholinesterase adduct: Insights into an aged-like inactive complex susceptible to reactivation by a combination of nucleophiles. (Pubmed Central) - Apr 13, 2024
The potent bulky reversible inhibitor 7-bis-tacrine (BTA) adopts, in the active site of the crystal structure of the MSF-enzyme adduct, a location and an orientation that closely resemble the one being found in the crystal structure of the BTA-enzyme complex...We show that the simultaneous presence of 2-PAM and the additional neutral oxime, 2-[(hydroxyimino)methyl]-l-methylimidazol (2-HAM), triggers the reactivation process of TcAChE within the hour timescale. Overall, our results pave the way toward the likely use of a cocktail of distinctive oximes as a promising recipe for an effective and fast reactivation of aged cholinesterases.
- | Cognex (tacrine) / Shionogi
Journal: A Sustainable Synthetic Approach to Tacrine and Cholinesterase Inhibitors in Deep Eutectic Solvents under Aerobic Conditions. (Pubmed Central) - Mar 28, 2024
Particularly notable is the synthesis of novel triazole-based derivatives, yielding 90-95%, by integrating an in situ preparation of aryl azides in DESs with N-propargyl-substituted tacrine derivatives. Quantitative metrics validate the green aspects of the reported drug development processes.
- | Cognex (tacrine) / Shionogi
Journal: New N-(1,3,4-thiadiazole-2-yl)acetamide derivatives as human carbonic anhydrase I and II and acetylcholinesterase inhibitors. (Pubmed Central) - Mar 27, 2024
Only compounds 6a and 6c showed superior activity against AChE compared to the standard agent, tacrine (THA). In silico studies, including absorption, distribution, metabolism and excretion (ADME) and drug-likeness evaluation, molecular docking, molecular dynamic simulations (MDSs) and density functional theory (DFT) calculations, were compatible with the in
- Myrbetriq (mirabegron) / Astellas, Cognex (tacrine) / Shionogi
Long-term Dementia Risk with Use of Anticholinergic versus Beta-3-Agonist Pharmacotherapy for Overactive Bladder (302A) - Mar 12, 2024 - Abstract #AUA2024AUA_3326;
In men, ACM were not associated with a higher risk relative to BA. These findings may reflect differences in the disease processes presenting with OAB and dementia risk between men and women.
- | Cognex (tacrine) / Shionogi
Journal: Multi-target potential of newly designed tacrine-derived cholinesterase inhibitors: Synthesis, computational and pharmacological study. (Pubmed Central) - Mar 11, 2024
Computationally predicted ADME properties indicated that these compounds should have good blood-brain barrier (BBB) permeability, an important factor for CNS-targeting drugs. Overall, all tested compounds showed promising pharmacological behavior, highlighting the multi-target potential of 2-chlorobenzoyl derivative which should be further investigated as a new lead in the drug development process.
- | Cognex (tacrine) / Shionogi
Journal: Protective Effects of Red Ginseng Against Tacrine-Induced Hepatotoxicity: An Integrated Approach with Network Pharmacology and Experimental Validation. (Pubmed Central) - Mar 4, 2024
In mice, RG also protected the liver injury induced by tacrine, as similar protective effects to silymarin, a well-known drug for liver toxicity protection. Our study reveals the potential of RG in mitigating tacrine-induced hepatotoxicity, suggesting the administration of natural products like RG to reduce toxicity in Alzheimer's disease treatment.
- | Cognex (tacrine) / Shionogi
Journal: Genomics and Drug Discovery Strategies: The Role of Natural Compounds and Its Receptor in Alzheimer's Disease. (Pubmed Central) - Feb 19, 2024
PTPN11 receptor with Carnosol ligand resulted in docking score (?G = -9.1 kcal/mol) w.r.t Tacrine (FDA drug) docked score (?G = -8.0 kcal/mol) followed by MD simulation. This research will aid in the identification of potential natural compounds that future researchers can use for further validation as a potential candidate drug in combating various neurodegenerative diseases highlighting AD.
- | ifenprodil tartrate / Chiba University Hospital
Journal: Phenoxytacrine derivatives: Low-toxicity neuroprotectants exerting affinity to ifenprodil-binding site and cholinesterase inhibition. (Pubmed Central) - Feb 5, 2024
Finally, compound I-52, showing only minor affinity to AChE, was identified as a lead candidate with favorable behavioral and neuroprotective effects using open-field and prepulse inhibition tests, along with scopolamine-based behavioral and NMDA-induced hippocampal lesion models. Our data show that compound I-52 exhibits low toxicity often associated with NMDA receptor ligands, and low hepatotoxicity, often related to THA-based compounds.
- | Cognex (tacrine) / Shionogi
Preclinical, Journal: In vitro and in vivo Biological Evaluation of Newly Tacrine-Selegiline Hybrids as Multi-Target Inhibitors of Cholinesterases and Monoamine Oxidases for Alzheimer's Disease. (Pubmed Central) - Feb 2, 2024
Lastly, 7d possessed well pharmacokinetic characteristics. In light of these results, it is clear that 7d could potentially serve as a promising multi-functional drug for the treatment of AD.
- | Cognex (tacrine) / Shionogi
Journal, IO biomarker: Structure Modification Converts the Hepatotoxic Tacrine into Novel Hepatoprotective Analogs. (Pubmed Central) - Jan 22, 2024
Furthermore, computer-assisted simulation docking results were highly consistent with those of the observed in vivo activities. In conclusion, the designed tacrine analogs exhibited a hepatoprotective role in acute liver damage, possibly through their antioxidative, anti-inflammatory, and antifibrotic effects.
- | Cognex (tacrine) / Shionogi
Journal: Design, synthesis and biological evaluation of carbamate derivatives incorporating multifunctional carrier scaffolds as pseudo-irreversible cholinesterase inhibitors for the treatment of Alzheimer's disease. (Pubmed Central) - Jan 17, 2024
In conclusion, the designed tacrine analogs exhibited a hepatoprotective role in acute liver damage, possibly through their antioxidative, anti-inflammatory, and antifibrotic effects. We used tacrine to modify the aliphatic substituent, and employed rivastigmine, indole and sibiriline fragments as carrier scaffolds...In the scopolamine-induced AD mouse model, C7 (20
- || Cognex (tacrine) / Shionogi
Review, Journal: Research and progress of focused ultrasound in the treatment of Alzheimer's disease. (Pubmed Central) - Jan 8, 2024
For the past few years, some studies could use focused ultrasound combined with microvesicles to induce blood brain barrier opening and targeted drug delivery to treat Alzheimer's disease, providing new opportunities for the treatment of Alzheimer's disease. This article reviews the application research and progress of focused ultrasound in the treatment of Alzheimer's disease, in order to provide new directions and ideas for the treatment of Alzheimer's disease.
- | Cognex (tacrine) / Shionogi
Journal: Design, synthesis, and biological evaluation of novel capsaicin-tacrine hybrids as multi-target agents for the treatment of Alzheimer's disease. (Pubmed Central) - Dec 17, 2023
This article reviews the application research and progress of focused ultrasound in the treatment of Alzheimer's disease, in order to provide new directions and ideas for the treatment of Alzheimer's disease. Moreover, compound 5s demonstrated good tolerance at the dose of up to 2500
- | Cognex (tacrine) / Shionogi
Journal: The synthesis, carbonic anhydrase and acetylcholinesterase inhibition effects of sulfonyl chloride moiety containing oxazolidinones using an intramolecular aza-Michael addition. (Pubmed Central) - Dec 15, 2023
Moreover, compound 5s demonstrated good tolerance at the dose of up to 2500 All the synthesized compounds had potent inhibition effects with Ki values in the range of 13.57?
- | Cognex (tacrine) / Shionogi
Journal: Piperazine-2-carboxylic acid derivatives as MTDLs anti-Alzheimer agents: Anticholinesterase activity, mechanistic aspect, and molecular modeling studies. (Pubmed Central) - Nov 28, 2023
In this regard, compound (7b) might be considered as a promising inhibitor of BChE with an innovative donepezil-based anti-Alzheimer activity. Further assessments of the most potent AChE and BChE inhibitors as potential MTDLs anti-Alzheimer's agents are under investigation with our research group and will be published later.
- | Cognex (tacrine) / Shionogi
Journal: Synthesis, biological evaluation, and computational studies of N-benzyl pyridinium-curcumin derivatives as potent AChE inhibitors with antioxidant activity. (Pubmed Central) - Nov 27, 2023
Further assessments of the most potent AChE and BChE inhibitors as potential MTDLs anti-Alzheimer's agents are under investigation with our research group and will be published later. Compound 7f, which had a benzyl moiety, showed the highest potency among all the target compounds, with an IC value of 7.5?
- | Cognex (tacrine) / Shionogi
Journal: Structural and molecular insights into tacrine-benzofuran hybrid induced inhibition of amyloid-? peptide aggregation and BACE1 activity. (Pubmed Central) - Nov 27, 2023
The MD simulations explain the observed high inhibitory activity of C1 against A? aggregation and BACE1 in the in
- | Cognex (tacrine) / Shionogi
Journal: Acetylcholinesterase inhibition of Alzheimer's disease: identification of potential phytochemicals and designing more effective derivatives to manage disease condition. (Pubmed Central) - Nov 27, 2023
Overall, this study was successful in finding new, highly effective, and possibly safer inhibitors of AChE. Communicated by Ramaswamy H. Sarma.
- Aduhelm (aducanumab) / Eisai, Biogen, Leqembi (lecanemab-irmb) / Biogen, BioArctic, Eisai, Cognex (tacrine) / Shionogi
A historical review of interventions for Alzheimer's disease (WCC Halls A-C) - Nov 3, 2023 - Abstract #Neuroscience2023NEUROSCIENCE_14220;
The literature indicates that these FDA-approved pharmacological interventions have modest effects in slowing the progression and symptoms of AD.However, controversy arose in 2021 when the FDA granted accelerated approval to aducanumab, the first monoclonal antibody treatment for AD...In 2023, lecanemab, another monoclonal antibody treatment, also received FDA accelerated approval, despite criticism concerning its efficacy and safety.Nevertheless, published data suggest that pharmacological treatments for AD are effective in treating symptoms of AD...Several studies have demonstrated that behavioral lifestyle modifications, such as aerobic exercises, can be a treatment recommendation for AD. For instance, physical exercise has long been recognized to promote improved memory function and cognitive health, presumably by protecting against hippocampal volume loss in older adults.Although there are significant advancements in developing treatment recommendations for AD, further research is warranted on the efficacy of AD treatments, including both pharmacotherapy and non-pharmacotherapy options.
- Cognex (tacrine) / Shionogi
Advancing Senescence-Based In Vitro Drug Testing for Alzheimer's Disease: Targeting A? and p-Tau Models in a Gut-Liver-Brain Multiorgan System (WCC Halls A-C) - Nov 3, 2023 - Abstract #Neuroscience2023NEUROSCIENCE_5948;
We will discuss the results of reduction in neuropathological burden and improvement in clinically relevant outcomes. Based on these considerations, we will establish the pathology of cellular senescence associated with p-tau and A-beta accumulation in AD and drug pretreatment utilizing the gut-liver-brain multiorgan system for AD drug discovery strategies.
- | Cognex (tacrine) / Shionogi
Preclinical, Journal: Antioxidant, LC-MS Analysis, and Cholinesterase Inhibitory Potentials of Phoenix dactylifera Cultivar Khudari: An In Vitro Enzyme Kinetics and In Silico Study. (Pubmed Central) - Oct 28, 2023
A molecular docking study exhibited that the compounds occupied the key residues of acetylcholinesterase with ?G range between -6.91 and -9.49 kcal/mol, where MDIE has ?G: -8.67 kcal/mol, which was better than that of tacrine, ?G: -8.25 kcal/mol...These findings suggest that the aqueous extract of Khudari fruit pulp has significant antioxidant and acetylcholinesterase inhibition potentials, and its compound, MDIE, forms stably with confirmation with the target protein, though this fruit of Khudari dates can be a better functional food for the treatment of Alzheimer's disease. Further investigations are needed to fully understand the therapeutic role of this plant-based compound via in vivo study.
- | Cognex (tacrine) / Shionogi
Journal: Structural and vibrational characterization of di-hydrated hydrochloride tacrine combining DFT with SQMFF approach. (Pubmed Central) - Oct 27, 2023
Both methods predict different assignments and scaled force constants presenting higher values those calculated with the wB97XD/6-311G* method. The predicted IR, Raman and H NMR spectra with both methods show good correlations with the corresponding experimental ones, however, better concordances between the C NMR and UV spectra are observed with the wB97XD/6-311G* method.
- | Cognex (tacrine) / Shionogi
Preclinical, Journal: Enzyme inhibitory potential of some indole Schiff bases on acetylcholinesterase and human carbonic anhydrase isoforms I and II enzymes: an in (Pubmed Central) - Oct 20, 2023
Compared to the control compound Tacrine (TAC), 1s showed the best inhibitory effect for AChE. In vitro results were verified with the results obtained by docking studies and interactions with enzymes were demonstrated.Communicated by Ramaswamy H. Sarma.
- || Cognex (tacrine) / Shionogi
Review, Journal: The effects of different acetylcholinesterase inhibitors on EEG patterns in patients with Alzheimer's disease: A systematic review. (Pubmed Central) - Oct 16, 2023
Also, differences between the effects of AChEIs on oligodendrocyte differentiation and myelination may be another important factor. This is the first article investigating the effect of different AChEIs on EEG patterns in patients with AD.
- | Cognex (tacrine) / Shionogi
Journal: Tacrine First-Phase Biotransformation and Associated Hepatotoxicity: A Possible Way to Avoid Quinone Methide Formation. (Pubmed Central) - Sep 18, 2023
The formation of Q-cysteine and Q-glutathione adducts after human liver microsome incubation was confirmed by all of the studied tacrine derivatives, but these findings were not confirmed after incubation with 3D PHH spheroids. Therefore, the presented data call into question the suggested previously hypothesized mechanism of toxicity, and the results open new avenues for chemical modifications to improve the safety of novel tacrine derivatives.
- | Cognex (tacrine) / Shionogi
Journal: Novel coumarin-chalcone derivatives: Synthesis, characterization, antioxidant, cyclic voltammetry, molecular modelling and biological evaluation studies as acetylcholinesterase, ?-glycosidase, and carbonic anhydrase inhibitors. (Pubmed Central) - Sep 18, 2023
Therefore, the presented data call into question the suggested previously hypothesized mechanism of toxicity, and the results open new avenues for chemical modifications to improve the safety of novel tacrine derivatives. Compounds 7c, 7e, 7g, 7i, 7j and 7l showed promising human carbonic anhydrase I inhibition compared to the standard Acetazolamide (K: 16.64
- | Cognex (tacrine) / Shionogi
Journal: Potential antioxidant, anticholinergic, antidiabetic and antiglaucoma activities and molecular docking of spiraeoside as a secondary metabolite of onion (Allium cepa). (Pubmed Central) - Sep 11, 2023
Spiraeoside demonstrated effective antioxidant, anticholinergic, antidiabetic and antiglaucoma activities. With these properties, it has shown that Spiraeoside has the potential to be a medicine for some metabolic diseases.
- || RGFP966 / BioMarin, tasquinimod (ABR-215050) / Active Biotech, Ipsen, Cognex (tacrine) / Shionogi
Review, Journal: Enhancement of neural regeneration as a therapeutic strategy for Alzheimer's disease (Review). (Pubmed Central) - Aug 24, 2023
However, further evaluations need to be performed to determine the optimal treatment. The present study reviews recent interventions for enhancing adult neurogenesis and attempts to elucidate their mechanisms of action, which may provide a theoretical basis for inducing nerve regeneration to fight against AD.
- || Aduhelm (aducanumab) / Eisai, Biogen, Leqembi (lecanemab-irmb) / Biogen, BioArctic, Eisai, Cognex (tacrine) / Shionogi
Review, Journal: Current and future therapeutic strategies for Alzheimer's disease: an overview of drug development bottlenecks. (Pubmed Central) - Aug 21, 2023
and anti-tau drugs, mitochondria-targeting and multi-targets, commercially available drugs, bottlenecks encountered in drug development, and the possible targets and therapeutic strategies for future drug development. We hope to present new concepts and methods for future drug therapies for AD.
- | Cognex (tacrine) / Shionogi
Journal: The Proof-of-Concept of MBA121, a Tacrine-Ferulic Acid Hybrid, for Alzheimer's Disease Therapy. (Pubmed Central) - Aug 16, 2023
plaque burden in the cerebral cortex and hippocampus in APP/PS1 transgenic male mice. Our in vivo results relate its bioavailability with the therapeutic response, demonstrating that MBA121 is a promising agent to treat the cognitive decline and neurodegeneration underlying AD.
- | Cognex (tacrine) / Shionogi
Journal: 1,2,3-Triazolo[4,5-b]aminoquinolines: Design, synthesis, structure, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity, and molecular docking of novel modified tacrines. (Pubmed Central) - Aug 14, 2023
Our in vivo results relate its bioavailability with the therapeutic response, demonstrating that MBA121 is a promising agent to treat the cognitive decline and neurodegeneration underlying AD. Specifically, 1,2,3-triazolo[4,5-b]aminoquinolines 5bb obtained from 3-methyl-carbonitrile (3b) showed the highest AChE (IC
- | Cognex (tacrine) / Shionogi
Preclinical, Journal: Novel beta-lactam substituted benzenesulfonamides: in (Pubmed Central) - Aug 4, 2023
Compounds 5f, 5h and 5l were also evaluated for their ability to inhibit the MCF-7 cancer cell line proliferation and were found to have promising anticancer activity, more potent than 5-fluorouracil and cisplatin...The acceptability of the compounds based on Lipinski's and Jorgensen's rules was also estimated from the ADME/T results. These results indicate that the synthesized molecules have the potential to be developed into effective and safe inhibitors of hCAs and AChE and could be lead agents.Communicated by Ramaswamy H. Sarma.
- | Cognex (tacrine) / Shionogi
Journal: Modified Tacrine Derivatives as Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Synthesis, Biological Evaluation, and Molecular Modeling Study. (Pubmed Central) - Jul 31, 2023
It was shown that 5c and 5d were blood-brain barrier (BBB) penetrants by online prediction. Taken together, these multifunctional properties highlight that compounds 5c and 5d can serve as promising candidates for the further development of multifunctional drugs against AD.
- | Cognex (tacrine) / Shionogi
Journal: Quinolinetrione-tacrine hybrids as multi-target-directed ligands against Alzheimer's disease. (Pubmed Central) - Jul 24, 2023
Importantly, 3 also showed low hepatotoxicity and good anti-amyloid aggregation properties. Remarkably, we uncovered the potential of the quinolinetrione scaffold, as a novel anti-amyloid aggregation and antioxidant motif to be used in further anti-AD MTDL drug discovery endeavors.
- | Cognex (tacrine) / Shionogi
Journal: Structural, harmonic force field and vibrational studies of cholinesterase inhibitor tacrine used for treatment of Alzheimer's disease. (Pubmed Central) - Jul 13, 2023
The gap values support the higher reactivity of form III while FB is the less reactive species in both media. Complete vibrational assignments for FB, CA and HCl species together with the corresponding scaled force constants are reported.
- | Cognex (tacrine) / Shionogi
Journal: Discovery of myrsinane-type Euphorbia diterpene derivatives through a skeleton conversion strategy from lathyrane diterpene for the treatment of Alzheimer's disease. (Pubmed Central) - Jul 10, 2023
Complete vibrational assignments for FB, CA and HCl species together with the corresponding scaled force constants are reported. In particular, derivative 37 displayed the most potent acetylcholinesterase (AChE) inhibition, with an IC value of 8.3
- donepezil / Generic mfg.
Investigating the role of Donepezil in promoting Oligodendrocyte precursor cell (OPC) differentiation and Therapeutic Potential in Alzheimer's Disease (AD). (Virtual) - Jul 6, 2023 - Abstract #AAIC2023AAIC_8053;
In particular, derivative 37 displayed the most potent acetylcholinesterase (AChE) inhibition, with an IC value of 8.3 Background: Statistical analysis of myelin basic protein (MBP) cells generated from Neural progenitor cell (NPC)-derived Oligodendrocyte precursor cells (OPCs) treated with various AChEIs, including donepezil, huperzine A, rivastigmine and tacrine, revealed that only donepezil is capable of facilitating OPC-to-OL formation, indicating that donepezil
- donepezil / Generic mfg.
Investigating the role of Donepezil in promoting Oligodendrocyte precursor cell (OPC) differentiation and Therapeutic Potential in Alzheimer's Disease (AD). (Virtual) - Jul 6, 2023 - Abstract #AAIC2023AAIC_5987;
Background: Statistical analysis of myelin basic protein (MBP) cells generated from Neural progenitor cell (NPC)-derived Oligodendrocyte precursor cells (OPCs) treated with various AChEIs, including donepezil, huperzine A, rivastigmine and tacrine, revealed that only donepezil is capable of facilitating OPC-to-OL formation, indicating that donepezil Background: Statistical analysis of myelin basic protein (MBP) cells generated from Neural progenitor cell (NPC)-derived Oligodendrocyte precursor cells (OPCs) treated with various AChEIs, including donepezil, huperzine A, rivastigmine and tacrine, revealed that only donepezil is capable of facilitating OPC-to-OL formation, indicating that donepezil
- donepezil / Generic mfg.
Investigating the role of Donepezil in promoting Oligodendrocyte precursor cell (OPC) differentiation and Therapeutic Potential in Alzheimer's Disease (AD). (Virtual) - Jul 6, 2023 - Abstract #AAIC2023AAIC_3741;
Background: Statistical analysis of myelin basic protein (MBP) cells generated from Neural progenitor cell (NPC)-derived Oligodendrocyte precursor cells (OPCs) treated with various AChEIs, including donepezil, huperzine A, rivastigmine and tacrine, revealed that only donepezil is capable of facilitating OPC-to-OL formation, indicating that donepezil Background: Statistical analysis of myelin basic protein (MBP) cells generated from Neural progenitor cell (NPC)-derived Oligodendrocyte precursor cells (OPCs) treated with various AChEIs, including donepezil, huperzine A, rivastigmine and tacrine, revealed that only donepezil is capable of facilitating OPC-to-OL formation, indicating that donepezil
- donepezil / Generic mfg.
Investigating the role of Donepezil in promoting Oligodendrocyte precursor cell (OPC) differentiation and Therapeutic Potential in Alzheimer's Disease (AD). (Virtual) - Jul 6, 2023 - Abstract #AAIC2023AAIC_1521;
Background: Statistical analysis of myelin basic protein (MBP) cells generated from Neural progenitor cell (NPC)-derived Oligodendrocyte precursor cells (OPCs) treated with various AChEIs, including donepezil, huperzine A, rivastigmine and tacrine, revealed that only donepezil is capable of facilitating OPC-to-OL formation, indicating that donepezil Background: Statistical analysis of myelin basic protein (MBP) cells generated from Neural progenitor cell (NPC)-derived Oligodendrocyte precursor cells (OPCs) treated with various AChEIs, including donepezil, huperzine A, rivastigmine and tacrine, revealed that only donepezil is capable of facilitating OPC-to-OL formation, indicating that donepezil
- | Cognex (tacrine) / Shionogi
Journal: Design, synthesis, biological evaluation and docking analysis of pyrrolidine-benzenesulfonamides as carbonic anhydrase or acetylcholinesterase inhibitors and antimicrobial agents. (Pubmed Central) - May 26, 2023
Background: Statistical analysis of myelin basic protein (MBP) cells generated from Neural progenitor cell (NPC)-derived Oligodendrocyte precursor cells (OPCs) treated with various AChEIs, including donepezil, huperzine A, rivastigmine and tacrine, revealed that only donepezil is capable of facilitating OPC-to-OL formation, indicating that donepezil Compounds 6a and 6b showed remarkable AChE inhibition effects with Ki values 22.34?
- | Cognex (tacrine) / Shionogi
Preclinical, Journal: Assessment of Anticholinergic and Antidiabetic Properties of Some Natural and Synthetic Molecules: an In Vitro and In Silico Approach. (Pubmed Central) - May 19, 2023
Compounds 6a and 6b showed remarkable AChE inhibition effects with Ki values 22.34? According to the results obtained, it may be said that the molecules used in the study are potential inhibitor candidates for AChE, BChE and ?-glycosidase.
- | Cognex (tacrine) / Shionogi
Journal: Exploring the Multitarget Activity of Wedelolactone against Alzheimer's Disease: Insights from In Silico Study. (Pubmed Central) - May 8, 2023
Furthermore, molecular docking simulations showed that the known forms of Wedelolactone at physiological pH effectively inhibited the AChE and BChE enzymes by comparing their activity to that of tacrine (control). Wedelolactone is a promising drug candidate for Alzheimer's disease therapy in light of these findings.
- | Cognex (tacrine) / Shionogi
Journal: Rapid discovery and crystallography study of highly potent and selective butylcholinesterase inhibitors based on oxime-containing libraries and conformational restriction strategies. (Pubmed Central) - Apr 5, 2023
With A2Q17 and A3Q12 as leads, a novel series of tacrine derivatives with nitrogen-containing heterocycles were designed based on conformation restriction strategy...X-ray crystallography structures of 39 or 43 complexes with BuChE revealed the molecular basis for their high potency. Thus, 39 and 43 are deserve for further study to develop potential drug candidates for the treatment of Alzheimer's disease.