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J Med Chem. 2015 Aug 27;58(16):6710-5. doi: 10.1021/acs.jmedchem.5b00958. Epub 2015 Aug 17.

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

Author information

1
Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, University of Jena , Philosophenweg 14, 07743 Jena, Germany.
2
Department of Pharmaceutical Biology, Institute of Pharmacy, University of Jena , Semmelweisstrasse 10, 07743 Jena, Germany.
3
Department of Anesthesiology, University Hospital of Ulm , Albert-Einstein-Allee 23, 89081 Ulm, Germany.
4
Institute of Pharmacy, Martin Luther University Halle-Wittenberg , Wolfgang-Langenbeck-Strasse 4, 06120 Halle/Saale, Germany.
5
Institute of Pharmacology and Toxicology, University of Jena , Drackendorfer Strasse 1, 07747 Jena, Germany.
6
Institute of Organic and Macromolecular Chemistry, Univerity of Jena , Humboldtstrasse 10, 07743 Jena, Germany.

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.

PMID:
26278660
DOI:
10.1021/acs.jmedchem.5b00958
[Indexed for MEDLINE]

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