Synthesis of a Series of Novel 3,9-Disubstituted Phenanthrenes as Analogues of Known M-Methyl-D-aspartate Receptor Allosteric Modulators.

Autor: Irvine, Mark W., Guangyu Fang, Eaves, Richard, Mayo-Martin, Maria B., Burnell, Erica S., Costa, Blaise M., Culley, Georgia R., Volianskis, Arturas, Collingridge, Graham L., Monaghanb, Daniel T., Jane, David E.
Předmět:
Zdroj: Synthesis; 2015, Vol. 47 Issue 11, p1593-1610, 18p
Abstrakt: 9-Substituted phenanthrene-3-carboxylic acids have been reported to have allosteric modulatory activity at the N-methyl-D-aspartate (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 in 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. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index