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
Citations
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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
Use of a 96-well microplate reader for measuring routine enzyme activities.
TL;DR: A method is described for the routine determination of the rate of colorimetric enzyme reactions using a 96-well microtiter plate reader commonly used in immunoassay and the interface with a personal computer allowed rapid manipulation of the absorbance values to calculate the desired rate data.
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In vitro effects of various cholinesterase inhibitors on acetyl- and butyrylcholinesterase of healthy volunteers.
TL;DR: L'activite de la physostigmine, the pyridostIGmine et the tacrine actuellement en phase d'essai clinique a egalement ete testee.
Journal ArticleDOI
THA--a review of the literature and its use in treatment of five overdose patients.
TL;DR: A review of the literature and its use in treatment of five overdose patients and the use of THA in Treatment of Five Overdose Patients in 1980 is published.