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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A Combined Chronic Low-Dose Soluble Epoxide Hydrolase and Acetylcholinesterase Pharmacological Inhibition Promotes Memory Reinstatement in Alzheimer’s Disease Mice Models
Júlia Jarné-Ferrer,Christian Griñán-Ferré,Aina Bellver-Sanchis,Santiago Vázquez,Diego Muñoz-Torrero,Mercè Pallàs +5 more
TL;DR: Results support the neuroprotectant role of chronic low-dose co-treatment strategy with sEH and AChE inhibitors in AD mouse models, opening new avenues for effective AD treatment.
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.