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
1,4-Substituted 4-(1H)-pyridylene-hydrazone-type inhibitors of AChE, BuChE, and amyloid-β aggregation crossing the blood-brain barrier.
Michaela Prinz,Sülünay Parlar,Gulsah Bayraktar,Vildan Alptüzün,Ercin Erciyas,Adyary Fallarero,Daniela Karlsson,Pia Vuorela,Malgorzata Burek,Carola Förster,Ezgi Turunc,Guliz Armagan,Ayfer Yalcin,Carola Schiller,Kristina Leuner,Manuel Krug,Christoph A. Sotriffer,Ulrike Holzgrabe +17 more
TL;DR: The bisnaphthyl substituted compound 20L was found to be the best overall inhibitor of AChE/BuChE and enhances the fibril destruction and blood-brain barrier mobility was ensured by a transwell assay.
Journal ArticleDOI
Donepezil (E2020): a new acetylcholinesterase inhibitor. Review of its pharmacology, pharmacokinetics, and utility in the treatment of Alzheimer’s disease
TL;DR: The results published to date suggest that donepezil will be a useful agent in the symptomatic treatment of Alzheimer's disease.
Journal ArticleDOI
Quantitative structure and bioactivity relationship study on human acetylcholinesterase inhibitors.
Aixia Yan,Kai Wang +1 more
TL;DR: Several QSAR (Quantitative Structure-Activity Relationships) models for predicting the inhibitory activity of 404 Acetylcholinesterase inhibitors were developed and a docking simulation was used to confirm the descriptors used.
Journal ArticleDOI
Reversible and irreversible inhibitory activity of succinic and maleic acid derivatives on acetylcholinesterase
José G. Trujillo-Ferrara,Iván Vázquez,Judith Espinosa,Rosa Santillan,Norberto Farfán,Herbert Höpfl +5 more
TL;DR: The conclusions of this study can be summarized as follows: (a) the aromatic moiety played a critical role in the recognition of the active site; (b) in case of the reversible inhibitor, there was an important increase in the affinity; and (c) the distance between phenolic hydroxyl and nitrogen was critical because the inhibition is ortho<
Journal ArticleDOI
Chlorinated tacrine analogs: Design, synthesis and biological evaluation of their anti-cholinesterase activity as potential treatment for Alzheimer's disease.
TL;DR: In this paper, a series of new 4-(chlorophenyl)tetrahydroquinoline derivatives, was synthesized and characterized and evaluated for their in vitro and in vivo anti-cholinesterase activity using tacrine as a reference standard.
References
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Journal ArticleDOI
Atomic structure of acetylcholinesterase from Torpedo californica: a prototypic acetylcholine-binding protein
Joel L. Sussman,Michal Harel,Felix Frolow,Christian Oefner,Adrian Goldman,Lilly Toker,Israel Silman +6 more
TL;DR: Modeling of acetylcholine binding to the enzyme suggests that the quaternary ammonium ion is bound not to a negatively charged "anionic" site, but rather to some of the 14 aromatic residues that line the gorge.
Journal ArticleDOI
Oral tetrahydroaminoacridine in long-term treatment of senile dementia, Alzheimer type.
TL;DR: It is suggested that THA may be at least temporarily useful in the long-term palliative treatment of patients with Alzheimer's disease, and further observations will be required before a clear assessment of the role of this agent can be made.
Journal ArticleDOI
A rapid, simple radiometric assay for cholinesterase, suitable for multiple determinations
TL;DR: A rapid and simple radiometric assay for cholinesterase, suitable for multiple determinations, has been developed, highly reproducible, quite sensitive, and useful for applications in which multiple samples must be quickly assayed.
Journal ArticleDOI
Mechanisms of cholinesterase inhibition in senile dementia of the alzheimer type: Clinical, pharmacological, and therapeutic aspects
Robert E. Becker,Ezio Giacobini +1 more
TL;DR: It is suggested that an adequate test of the efficacy of ChE inhibition may await the use of new and improved ChE inhibitors that produce significantly fewer side effects and greater therapeutic effects than drugs presently being tested for efficacy in the treatment of SDAT patients.
Journal ArticleDOI
9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics.
Gregory M. Shutske,Pierrat Frank A,Kevin J. Kapples,Michael Cornfeldt,Mark R. Szewczak,Francis P. Huger,Gina M. Bores,Vahram Haroutunian,Kenneth L. Davis +8 more
TL;DR: These compounds are related to 1,2,3,4-tetrahydro-9-acridinamine and inhibit acetylcholinesterase in vitro and are active in a model that may be predictive of activity in Alzheimer's disease--the scopolamine-induced impairment of 24-h memory of a passive dark-avoidance paradigm in mice.