Synthesis of a Series of Novel 3,9-Disubstituted Phenanthrenes as Analogues of Known NMDA Receptor Allosteric Modulators

9-Substituted phenanthrene-3-carboxylic acids have been reported to have allosteric modulatory activity at the NMDA receptor. This receptor is activated by the excitatory neurotransmitter L-glutamate and has been implicated in a range of neurological disorders such as schizophrenia, epilepsy and chr...

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Veröffentlicht in:Synthesis (Stuttgart) 2015-06, Vol.47 (11), p.1593-1610
Hauptverfasser: Irvine, Mark W, Fang, Guangyu, Eaves, Richard, Mayo-Martin, Maria B, Burnell, Erica S, Costa, Blaise M, Culley, Georgia R, Volianskis, Arturas, Collingridge, Graham L, Monaghan, Daniel T, Jane, David E
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Sprache:eng
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Zusammenfassung:9-Substituted phenanthrene-3-carboxylic acids have been reported to have allosteric modulatory activity at the NMDA receptor. This receptor is activated by the excitatory neurotransmitter L-glutamate and has been implicated in a range of neurological disorders such as schizophrenia, epilepsy and chronic pain and neurodegenerative disorders such as Alzheimer's disease. Herein, the convenient synthesis of a wide range of novel 3,9-disubstituted phenanthrene derivatives starting from a few common intermediates is described. These new phenanthrene derivatives will help to clarify the structural requirements for allosteric modulation of the NMDA receptor.
ISSN:0039-7881
1437-210X
DOI:10.1055/s-0034-1380114