Cognex (tacrine) / Shionogi 
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  • ||||||||||  Cognex (tacrine) / Shionogi
    Review, Journal:  Chromenone: An emerging scaffold in anti-Alzheimer drug discovery. (Pubmed Central) -  Aug 14, 2024   
    Natural chromenone, quercetin, scopoletin, esculetin, coumestrol, umbelliferone, bergapten, and methoxsalen (xanthotoxin), and synthetic chromenone hybrids comprising structures like acridine, 4-aminophenyl, 3-arylcoumarins, quinoline, 1,3,4-oxadiazole, 1,2,3-triazole, and tacrine, have been explored for their potential to combat AD...This review comprehensively explores natural, semisynthetic, and synthetic chromenone, elucidating their synthetic routes, possible mode of action/drug targets and structure-activity relationships (SAR). The acquired knowledge provides valuable insights for the development of new chromenone hybrids against AD.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Journal, Metabolomic study:  Applying Spatial Metabolomics To Investigate Age- and Drug-Induced Neurochemical Changes. (Pubmed Central) -  Jul 29, 2024   
    An age-dependent increase in the glutamine/glutamate ratio, an indicator of glia-neuron interconnection and neurotoxicity, was detected after tacrine administration. The presented metabolic mapping approach was able to provide visualizations of the lipid signaling and neurotransmission alterations induced by early aging and can thus be beneficial to further elucidating age-related neurochemical pathways.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Preclinical, Journal:  Selenylated Analogs of Tacrine: Synthesis, in Silico and in Vitro (Pubmed Central) -  Jul 10, 2024   
    In vitro studies elucidated the antioxidant effects of Tacrine and its selenium hybrid (TSe) in neutralizing ABTS radicals, scavenging DPPH radicals, and reducing iron ions. Additionally, the acute oral toxicity of one synthesized compound was evaluated.
  • ||||||||||  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:  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:  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
    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
    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.
  • ||||||||||  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
    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
    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.
  • ||||||||||  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
    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:  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.