Journal ArticleDOI
The synthesis and in vitro acetylcholinesterase and butyrylcholinesterase inhibitory activity of tacrine (Cognex®) derivaties
TLDR
Chlorosubstituted derivatives of tacrine, 1,4-methylenetacrine, and their in vitro acetylcholinesterase and butyrylcholiersterase inhibitory activities are described.About:
This article is published in Bioorganic & Medicinal Chemistry Letters.The article was published on 1992-08-01. It has received 46 citations till now. The article focuses on the topics: Tacrine & Butyrylcholinesterase.read more
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Journal ArticleDOI
Recent Advances in the Friedländer Reaction
José Marco-Contelles,Elena Pérez-Mayoral,Abdelouahid Samadi,Maria do Carmo Carreiras,Elena Soriano +4 more
Journal ArticleDOI
Research and development of donepezil hydrochloride, a new type of acetylcholinesterase inhibitor.
TL;DR: Donepezil showed several positive characteristics including the following: It has a novel structure compared to other conventional ChE inhibitors; it shows strong anti-AChE activity and has long lasting efficacy; the inhibitory characteristic of donepezil shows that it is highly selective for AChE as compared to butyrylcholinesterase (BuChE) and showed reversibility.
Journal ArticleDOI
Targeting acetylcholinesterase to treat neurodegeneration.
TL;DR: The development of bivalent ligands that occupy both the active and the peripheral site of AChE might be more beneficial for treatment of Alzheimer´s disease than simple inhibition of the acetylcholine hydrolysis.
Journal ArticleDOI
Pyrano[3,2-c]quinoline−6-Chlorotacrine Hybrids as a Novel Family of Acetylcholinesterase- and β-Amyloid-Directed Anti-Alzheimer Compounds
Pelayo Camps,Xavier Formosa,Carles Galdeano,Diego Muñoz-Torrero,Lorena Ramírez,Elena Gómez,Nicolas Isambert,Rodolfo Lavilla,Albert Badia,M. Victòria Clos,Manuela Bartolini,Francesca Mancini,Vincenza Andrisano,Mariana P. Arce,M. Isabel Rodríguez-Franco,Oscar Huertas,Thomai Dafni,F. Javier Luque +17 more
TL;DR: Two isomeric series of dual binding site acetylcholinesterase (AChE) inhibitors that retain the potent and selective human AChE inhibitory activity of the parent 6-chlorotacrine while exhibiting a significant in vitro inhibitoryActivity toward the AChe-induced and self-induced Abeta aggregation and toward BACE-1, as well as ability to enter the central nervous system, which makes them promising anti-Alzheimer lead compounds.
Journal ArticleDOI
SAR of 9-Amino-1,2,3,4-tetrahydroacridine-Based Acetylcholinesterase Inhibitors: Synthesis, Enzyme Inhibitory Activity, QSAR, and Structure-Based CoMFA of Tacrine Analogues
Maurizio Recanatini,Andrea Cavalli,Federica Belluti,Lorna Piazzi,Angela Rampa,Alessandra Bisi,Silvia Gobbi,Piero Valenti,Vincenza Andrisano,Manuela Bartolini,Vanni Cavrini +10 more
TL;DR: This study attempted to derive a comprehensive SAR picture for the class of acetylcholinesterase (AChE) inhibitors related to tacrine, a drug currently in use for the treatment of the Alzheimer's disease.
References
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Journal ArticleDOI
Enzyme inhibiting action of tetrahydroaminoacridine and its structural fragments
TL;DR: Tetrahydro‐5‐aminoacridine and four compounds representing its structural fragments have been compared as inhibitors of acetylcholinesterase and of monoamine oxidase, and 4‐Arninoquinoline shows a stronger monoamines oxidase inhibition than any known therapeutically used inhibitor.
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Role of butyrylcholinesterase in canine tracheal smooth muscle function
TL;DR: BuChE serves to coregulate the lifetime of ACh in canine tracheal smooth muscle by inhibiting ChE activity with little or no effect on AChE activity.
Journal Article
Interaction of tetrahydroaminoacridine with acetylcholinesterase and butyrylcholinesterase.
Harvey Alan Berman,K Leonard +1 more
TL;DR: In this paper, tetrahydroaminoacridine (THA) was shown to associate with AchE and BuchE with high affinity and that subsequent inhibition comes about through ligand association at the active center rather than at a peripheral site.
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Differentiation and distribution of acetylcholinesterase molecular forms in the mouse cochlea.
M.R Emmerling,Hanna M. Sobkowicz +1 more
TL;DR: The results indicate that in the cochlea the content of molecular forms is similar to that of other neuronal systems, the expression of AChE Molecular forms is developmentally regulated, and the ACh E isoenzymes develop and are distributed differentially along the coChlear length; resulting near maturity in the greater proportional expression of G4 and A12 in the base and midturn and G2/G1 in the apex.
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Tetrahydroaminoacridine in Alzheimer's dementia: Clinical and biochemical results of a double-blind crossover trial
TL;DR: The results indicate that THA has a therapeutic potential, although its pharmacokinetic profile and its liability to induce liver damage may limit the clinical use of the drug in the future.