Evaluation of Homobivalent Carbolines as Designed Multiple Ligands for the Treatment of Neurodegenerative Disorders
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- 作者：Robert Otto ; Robert Penzis ; Friedemann Gaube ; Oliver Adolph ; Karl J. F枚hr ; Paul Warncke ; Dina Robaa ; Dorothea Appenroth ; Christian Fleck ; Christoph Enzensperger ; Jochen Lehmann ; Thomas Winckler
- 刊名：Journal of Medicinal Chemistry
- 出版年：2015
- 出版时间：August 27, 2015
- 年：2015
- 卷：58
- 期：16
- 页码：6710-6715
- 全文大小：272K
- ISSN：1520-4804
文摘
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 纬-carbolinium salts as potent inihitors of both cholinesterases, N-methyl-d-aspartate receptors, and monoamine oxidases. Homobivalent 纬-carbolines displayed similar structure鈥揳ctivity relationships on all tested targets and may present promising designed multiple ligands for the treatment of neurodegenerative disorders.