title: Synthesis of a Series of Novel 3,9-Disubstituted Phenanthrenes as Analogues of Known NMDA Receptor Allosteric Modulators.
abstract: 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.
authors.affiliation: School of Physiology & Pharmacology, Medical Sciences Building, University Walk, University of Bristol, Bristol, BS8 1TD, UK.
authors.forename: Mark W
authors.initials: MW
authors.lastname: Irvine
authors.affiliation: School of Physiology & Pharmacology, Medical Sciences Building, University Walk, University of Bristol, Bristol, BS8 1TD, UK.
authors.forename: Guangyu
authors.initials: G
authors.lastname: Fang
authors.affiliation: School of Physiology & Pharmacology, Medical Sciences Building, University Walk, University of Bristol, Bristol, BS8 1TD, UK.
authors.forename: Richard
authors.initials: R
authors.lastname: Eaves
authors.affiliation: School of Physiology & Pharmacology, Medical Sciences Building, University Walk, University of Bristol, Bristol, BS8 1TD, UK.
authors.forename: Maria B
authors.initials: MB
authors.lastname: Mayo-Martin
authors.affiliation: School of Physiology & Pharmacology, Medical Sciences Building, University Walk, University of Bristol, Bristol, BS8 1TD, UK.
authors.forename: Erica S
authors.initials: ES
authors.lastname: Burnell
authors.affiliation: Department of Pharmacology and Experimental Neuroscience, University of Nebraska Medical Center, Omaha, Nebraska 68198-6260 U.S.A.
authors.forename: Blaise M
authors.initials: BM
authors.lastname: Costa
authors.affiliation: School of Physiology & Pharmacology, Medical Sciences Building, University Walk, University of Bristol, Bristol, BS8 1TD, UK.
authors.forename: Georgia R
authors.initials: GR
authors.lastname: Culley
authors.affiliation: School of Physiology & Pharmacology, Medical Sciences Building, University Walk, University of Bristol, Bristol, BS8 1TD, UK.
authors.forename: Arturas
authors.initials: A
authors.lastname: Volianskis
authors.affiliation: School of Physiology & Pharmacology, Medical Sciences Building, University Walk, University of Bristol, Bristol, BS8 1TD, UK.
authors.forename: Graham L
authors.initials: GL
authors.lastname: Collingridge
authors.affiliation: Department of Pharmacology and Experimental Neuroscience, University of Nebraska Medical Center, Omaha, Nebraska 68198-6260 U.S.A.
authors.forename: Daniel T
authors.initials: DT
authors.lastname: Monaghan
authors.affiliation: School of Physiology & Pharmacology, Medical Sciences Building, University Walk, University of Bristol, Bristol, BS8 1TD, UK.
authors.forename: David E
authors.initials: DE
authors.lastname: Jane
keywords: NMDA receptor; Phenanthrenes; Wittig reaction; allosteric modulators; palladium coupling