Combined Strategies for the Discovery of Ionotropic Glutamate Receptor Antagonists

被引：14

作者：

Chimirri, Alba ^{[1
]}

De Luca, Laura ^{[1
]}

Ferro, Stefania ^{[1
]}

De Sarro, Giovanbattista ^{[2
]}

Ciranna, Lucia ^{[3
]}

Gitto, Rosaria ^{[1
]}

机构：

[1] Univ Messina, Dipartimento Farmacochim, I-98168 Messina, Italy

[2] Magna Graecia Univ Catanzaro, Dipartimento Med Sperimentale & Clin, I-88100 Catanzaro, Italy

[3] Univ Catania, Dipartimento Sci Fisiol, I-95125 Catania, Italy

来源：

CHEMMEDCHEM | 2009年 / 4卷 / 06期

关键词：

AMPA; antagonists; molecular modeling; NR213/NMDA; receptors; AMPA RECEPTOR; NR2B SUBUNIT; PHARMACOLOGICAL-PROPERTIES; ANTICONVULSANT ACTIVITY; NMDA; DERIVATIVES; MODELS; TARGET;

D O I：

10.1002/cmdc.200900109

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This review summarizes the results of our research group engaged in the development of new glutamate receptor ligands. Chemical and biological studies of several active molecules have been carried out. In particular, extensive work has addressed the identification of antagonists of AMPA and NMDA receptor subtypes using a combination of computational strategies. Innovative synthetic pathways have been used and small libraries of new molecules prepared. In vitro and in vivo tests were performed, and some compounds proved to be highly potent anticonvulsant and neuroprotective agents.

引用

页码：917 / 922

页数：6

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