Synthesis of a Series of Novel 3,9-Disubstituted Phenanthrenes as Analogues of Known NMDA Receptor Allosteric Modulators.
Synthesis of a Series of Novel 3,9-Disubstituted Phenanthrenes as Analogues of Known NMDA Receptor Allosteric Modulators.
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DOI：
10.1055/s-0034-1380114
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发表时间：
2015-06-01
期刊：
影响因子：
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通讯作者：
Jane DE
中科院分区：
文献类型：
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作者：
Irvine MW;Fang G;Eaves R;Mayo-Martin MB;Burnell ES;Costa BM;Culley GR;Volianskis A;Collingridge GL;Monaghan DT;Jane DE
9-据报道，取代的菲-3-羧酸对NMDA受体具有变构调节活性。该受体被兴奋性神经递质L-谷氨酸激活，并且与一系列神经系统疾病如精神分裂症、癫痫和慢性疼痛以及神经退行性疾病如阿尔茨海默病有关。本文介绍了从几种常见的中间体出发，方便地合成一系列新颖的3，9-二取代菲衍生物的方法。这些新的菲衍生物将有助于阐明NMDA受体变构调节的结构要求。3，9-二取代菲
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. 3,9-Disubstituted Phenanthrenes