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Evaluation of Homobivalent Carbolines as Designed Multiple Ligands for the Treatment of Neurodegenerative Disorders.

Authors :
Otto R
Penzis R
Gaube F
Adolph O
Föhr KJ
Warncke P
Robaa D
Appenroth D
Fleck C
Enzensperger C
Lehmann J
Winckler T
Source :
Journal of medicinal chemistry [J Med Chem] 2015 Aug 27; Vol. 58 (16), pp. 6710-5. Date of Electronic Publication: 2015 Aug 17.
Publication Year :
2015

Abstract

Neurodegenerative diseases represent a challenge for biomedical research due to their high prevalence and lack of mechanism-based treatments. Because of the complex pathology of neurodegenerative disorders, multifunctional drugs have been increasingly recognized as potential treatments. We identified homobivalent γ-carbolinium salts as potent inihitors of both cholinesterases, N-methyl-D-aspartate receptors, and monoamine oxidases. Homobivalent γ-carbolines displayed similar structure-activity relationships on all tested targets and may present promising designed multiple ligands for the treatment of neurodegenerative disorders.

Details

Language :
English
ISSN :
1520-4804
Volume :
58
Issue :
16
Database :
MEDLINE
Journal :
Journal of medicinal chemistry
Publication Type :
Academic Journal
Accession number :
26278660
Full Text :
https://doi.org/10.1021/acs.jmedchem.5b00958