Novel diarylated tacrine derivatives: Synthesis, characterization, anticancer, antiepileptic, antibacterial, and antifungal activities
Sign Up to like & getrecommendations! Published in 2024 at "Journal of Biochemical and Molecular Toxicology"
DOI: 10.1002/jbt.23706
Abstract: In this study, our goal was to synthesize novel aryl tacrine derivatives and assess their potential as anticancer, antibacterial agents, and enzyme inhibitors. We adopted a two‐step approach, initiating with the synthesis of dibromotacrine derivatives… read more here.
Keywords: novel diarylated; anticancer; diarylated tacrine; characterization ... See more keywords
Intracellular distribution of new tacrine analogues as a potential cause of their cytotoxicity against human neuroblastoma cells SH-SY5Y
Sign Up to like & getrecommendations! Published in 2018 at "Medicinal Chemistry Research"
DOI: 10.1007/s00044-018-2241-6
Abstract: Four new glyco-conjugated tacrine derivatives, 4-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl)-1-(1,2,3,4-tetrahydroacridin-9-yl)thiosemicarbazide (1), 4-(2,3,4,6-tetra-O-acetyl-β-D-mannopyranosyl)-1-(1,2,3,4-tetrahydroacridin-9-yl)thiosemicarbazide (2), 2′-(1,2,3,4-tetrahydroacridin-9-yl)hydrazono-3′-(2,3,4,6-tetra-O-acetyl-β-D-galactopyranosyl)-1′,3′-thiazolidin-4′-one (3) and [2′-(1,2,3,4-tetrahydro-acridin-9-yl)hydrazono-3′-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl)-4′-oxothiazolidin-5-yliden]acetate (4) were synthesized and their characteristics were investigated. All of the novel derivatives were found to inhibit acetylcholinesterase obtained from Electrophorus electricus… read more here.
Keywords: human neuroblastoma; tetra acetyl; cytotoxicity; neuroblastoma cells ... See more keywords
Design, synthesis and biological activity of novel tacrine-isatin Schiff base hybrid derivatives.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2019.103006
Abstract: A series of novel tacrine-isatin Schiff base hybrid derivatives (7a-p) were designed, synthesized and evaluated as multi-target candidates against Alzheimer's disease (AD). The biological assays indicated that most of these compounds displayed potent inhibitory activity… read more here.
Keywords: ache; tacrine isatin; isatin schiff; tacrine ... See more keywords
A review on tacrine-based scaffolds as multi-target drugs (MTDLs) for Alzheimer's disease.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2016.10.060
Abstract: Alzheimer's disease (AD) is a multifactorial neurological disorder among elderly people and combinatorial factors such as genetic, lifestyle, and environmental are involved in onset and disease progression. It has been demonstrated that loss of cholinergic… read more here.
Keywords: tacrine based; based scaffolds; alzheimer disease; disease ... See more keywords
Dimeric Tacrine(10)-hupyridone as a Multitarget-Directed Ligand To Treat Alzheimer's Disease.
Sign Up to like & getrecommendations! Published in 2021 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.1c00182
Abstract: Alzheimer's disease (AD) is a neurodegenerative disorder with multiple pathological features. Therefore, a multitarget-directed ligands (MTDLs) strategy has been developed to treat AD. We have previously designed and synthesized dimeric tacrine(10)-hupyridone (A10E), a novel tacrine… read more here.
Keywords: alzheimer disease; a10e could; dimeric tacrine; a10e ... See more keywords
Polymer drug conjugates containing memantine, tacrine and cinnamic acid: promising nanotherapeutics for the treatment of Alzheimer’s disease
Sign Up to like & getrecommendations! Published in 2023 at "Journal of Microencapsulation"
DOI: 10.1080/02652048.2023.2167011
Abstract: Abstract Aim To prepare polymer-drug conjugates containing a combination of memantine, tacrine, and E)-N-(3-aminopropyl)cinnamide, promising therapeutics for the treatment of neurodegenerative disorders. Methods The conjugates were characterised by 1HNMR, particle size analysis, SEM, LC-MS, TEM/EDX,… read more here.
Keywords: polymer drug; tacrine; drug conjugates; memantine tacrine ... See more keywords
Investigation of the enantioselectivity of acetylcholinesterase and butyrylcholinesterase upon inhibition by tacrine-iminosugar heterodimers
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2022.2150762
Abstract: Abstract The copper-catalysed azide-alkyne cycloaddition was applied to prepare three enantiomeric pairs of heterodimers containing a tacrine residue and a 1,4-dideoxy-1,4-imino-D-arabinitol (DAB) or 1,4-dideoxy-1,4-imino-L-arabinitol (LAB) moiety held together via linkers of variable lengths containing a… read more here.
Keywords: tacrine; inhibition; investigation enantioselectivity; enantioselectivity acetylcholinesterase ... See more keywords
Protective Effects of Red Ginseng Against Tacrine-Induced Hepatotoxicity: An Integrated Approach with Network Pharmacology and Experimental Validation
Sign Up to like & getrecommendations! Published in 2024 at "Drug Design, Development and Therapy"
DOI: 10.2147/dddt.s450305
Abstract: Introduction Tacrine, an FDA-approved acetylcholinesterase inhibitor, has shown efficacy in treating Alzheimer’s disease, but its clinical use is limited by hepatotoxicity. This study investigates the protective effects of red ginseng against tacrine-induced hepatotoxicity, focusing on… read more here.
Keywords: protective effects; tacrine induced; pharmacology; induced hepatotoxicity ... See more keywords
Therapeutic Potential of Multifunctional Tacrine Analogues
Sign Up to like & getrecommendations! Published in 2019 at "Current Neuropharmacology"
DOI: 10.2174/1570159x16666180412091908
Abstract: Abstract: Tacrine is a potent inhibitor of cholinesterases (acetylcholinesterase and butyrylcholinesterase) that shows limiting clinical application by liver toxicity. In spite of this, analogues of tacrine are considered as a model inhibitor of cholinesterases in… read more here.
Keywords: therapeutic potential; tacrine analogues; tacrine; alzheimer disease ... See more keywords
Design, Synthesis and Molecular Modeling Study of Radiotracers Based on Tacrine and Its Derivatives for Study on Alzheimer’s Disease and Its Early Diagnosis
Sign Up to like & getrecommendations! Published in 2024 at "Applied Sciences"
DOI: 10.3390/app14072827
Abstract: From 1993 to 2013, tacrine was an approved drug for Alzheimer’s disease. Due to its strong inhibitory properties towards cholinesterase, tacrine causes an increase in the level of the neurotransmitter acetylcholine in the cholinergic system… read more here.
Keywords: alzheimer disease; diagnosis; based tacrine; tacrine derivatives ... See more keywords