Huprine derivatives as sub-nanomolar human acetylcholinesterase inhibitors: from rational design to validation by X-ray crystallography

ChemMedChem. 2012 Mar 5;7(3):400-5. doi: 10.1002/cmdc.201100438. Epub 2011 Nov 4.

Authors

Cyril Ronco¹, Eugénie Carletti, Jacques-Philippe Colletier, Martin Weik, Florian Nachon, Ludovic Jean, Pierre-Yves Renard

Affiliation

¹ Equipe de Chimie Bio-organique, COBRA-CNRS UMR 6014 & FR 3038, Rue Lucien Tesnière, 76131 Mont-Saint-Aignan, France.

PMID: 22052791
DOI: 10.1002/cmdc.201100438

No abstract available

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Acetylcholinesterase / metabolism*
Alzheimer Disease / drug therapy
Alzheimer Disease / enzymology
Aminoquinolines / chemical synthesis*
Aminoquinolines / pharmacology
Animals
Brain / drug effects
Brain / enzymology
Cholinesterase Inhibitors / chemical synthesis*
Cholinesterase Inhibitors / pharmacology
Crystallography, X-Ray
Dogs
Heterocyclic Compounds, 4 or More Rings / chemical synthesis*
Heterocyclic Compounds, 4 or More Rings / pharmacology
Humans
Models, Molecular
Solutions
Stereoisomerism
Thermodynamics

Substances

Aminoquinolines
Cholinesterase Inhibitors
Heterocyclic Compounds, 4 or More Rings
Solutions
huprine X
huprine Y
Acetylcholinesterase