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Development of coumarin-inspired bifunctional hybrids as a new class of anti-Alzheimer's agents with potent efficacy.
RSC Med Chem
December 2024
Department of Pharmaceutical Sciences, Guru Nanak Dev University Amritsar Punjab 143005 India
Considering the multifactorial and complex nature of Alzheimer's disease and the requirement of an optimum multifunctional anti-Alzheimer's agent, a series of triazole tethered coumarin-eugenol hybrid molecules was designed as potential multifunctional anti-Alzheimer's agents using donepezil and a template. The designed hybrid molecules were synthesized a click chemistry approach and preliminarily screened for cholinesterase and Aβ aggregation inhibition. Among them, AS15 emerged as a selective inhibitor of AChE (IC = 0.
View Article and Find Full Text PDFHydroxyl chalcone derivative DK02 as a multi-target-directed ligand for Alzheimer's disease: A preclinical study in zebrafish.
Br J Pharmacol
December 2024
Toxicology and Pharmacology Laboratory, Department of Biotechnology, Faculty of Science and Humanities, SRM Institute of Science and Technology, Kattankulathur, Tamil Nadu, India.
Background And Purpose: Alzheimer's disease (AD) is a widespread neurodegenerative condition characterized by amyloid-beta (Aβ) plaques and tau protein aggregates, leading to significant cognitive decline. Existing treatments primarily offer symptomatic relief, underscoring the urgent need for novel therapies that address multiple AD pathways. This study evaluates the efficacy of DK02, a hydroxyl chalcone derivative, in a scopolamine-induced dementia model in zebrafish, hypothesizing that it targets several neurodegenerative mechanisms simultaneously.
View Article and Find Full Text PDFThe impact of mGlu2 or mGlu5 receptor activators on the production of l-arginine derivatives and the expression of PRMT5 or DDAH1 enzymes in animal models of cognitive decline.
Nitric Oxide
February 2025
Maj Institute of Pharmacology Polish Academy of Sciences, 12 Smetna Street, 31-343, Krakow, Poland. Electronic address:
l-arginine derivatives (ADMA, SDMA, NMMA) are endogenous inhibitors of nitric oxide (NO֗) production, which is essential in critical brain processes including blood-brain barrier (BBB) integrity and long-term potentiation (LTP). ADMA and NMMA are degraded by dimethylarginine dimethylaminohydrolase 1 (DDAH1) and protein arginine methyltransferase 5 (PRMT5) is an emerging epigenetic enzyme that mainly represses transcription of target genes via symmetric dimethylation of arginine residues. There is no data concerning the impact of metabotropic glutamate receptors (mGlu) ligands on this aspect of brain physiology.
View Article and Find Full Text PDFA comprehensive analysis of in-hospital adverse events after scopolamine administration: insights from a retrospective cohort study using a large nationwide inpatient database.
BMC Anesthesiol
November 2024
Department of Anesthesiology and Perioperative Medicine, Thomas Jefferson University, 111 S 11th St Gibbon Building, Philadelphia, PA, 8330, 19107, USA.
Background: Scopolamine is a widely used antiemetic in anesthetic practice, particularly for postoperative and post-discharge nausea and vomiting. Despite its frequent usage and recognized efficacy, concerns have emerged regarding the potential for increased side effects, particularly in elderly patients. Further research is needed to assess safety and determine age thresholds for adverse events.
View Article and Find Full Text PDFDiscovery of novel thiosemicarbazone-acridine targeting butyrylcholinesterase with antioxidant, metal complexing and neuroprotector abilities as potential treatment of Alzheimer's disease: In vitro, in vivo, and in silico studies.
Eur J Med Chem
January 2025
Institute of Chemistry, Universidade Federal Rural do Rio de Janeiro, Seropédica, 23897-000, Brazil. Electronic address:
Inhibition of cholinesterases, combined with antioxidant activity, metal-chelating capacity, and neuroprotection, is recognized as an effective multitarget therapy for the treatment of Alzheimer's disease (AD). Based on our in-house thiosemicarbazone-acridine compounds, this study recognized these derivatives as possible multi-target-directed ligand (MTDL). Initial screening against cholinesterases identified CL-01, which exhibited a promising IC value of 0.
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