Novel and potent tacrine-related hetero- and homobivalent ligands for acetylcholinesterase and butyrylcholinesterase

Based upon synthetic and biochemical results, a novel and potent tacrine analogue and heterobivalent analogues of tacrine, were designed. The role played by the amino groups of homo- and heterobivalent ligands in the interaction with the peripheral and catalytic sites of AChE and BuChE were investig...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2001-07, Vol.11 (13), p.1779-1782
Main Authors: Savini, Luisa, Campiani, Giuseppe, Gaeta, Alessandra, Pellerano, Cesare, Fattorusso, Caterina, Chiasserini, Luisa, Fedorko, James M, Saxena, Ashima
Format: Article
Language:English
Subjects:
Acetylcholinesterase - chemistry
Acetylcholinesterase - metabolism
Biological and medical sciences
Butyrylcholinesterase - chemistry
Butyrylcholinesterase - metabolism
Catalytic Domain
Ligands
Medical sciences
Neuropharmacology
Pharmacology. Drug treatments
Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease)
Psychology. Psychoanalysis. Psychiatry
Psychopharmacology
Tacrine - chemistry
Tacrine - metabolism
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Based upon synthetic and biochemical results, a novel and potent tacrine analogue and heterobivalent analogues of tacrine, were designed. The role played by the amino groups of homo- and heterobivalent ligands in the interaction with the peripheral and catalytic sites of AChE and BuChE were investigated. The syntheses of these materials together with the results of AChE/BuChE inhibition assays are detailed. Graphic
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00294-3