Synthesis of a Series of Novel 3,9-Disubstituted Phenanthrenes as Analogues of Known N-Methyl-d-aspartate Receptor Allosteric Modulators

Author:

Irvine Mark1,Fang Guangyu1,Eaves Richard1,Mayo-Martin Maria1,Burnell Erica1,Costa Blaise2,Culley Georgia1,Volianskis Arturas1,Collingridge Graham1,Monaghan Daniel2,Jane David1

Affiliation:

1. School of Physiology and Pharmacology, Medical Sciences Building, University Walk, University of Bristol

2. Department of Pharmacology and Experimental Neuroscience, University of Nebraska Medical Center

Abstract

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.

Publisher

Georg Thieme Verlag KG

Subject

Organic Chemistry,Catalysis

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