Development of 3-substituted-1H
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- 作者：Rosaria Gitto ; Laura De Luca ; Stefania Ferro ; Rita Citraro ; Giovambattista De Sarro ; Lara Costa ; Lucia Ciranna ; Alba Chimirri
- 关键词：NR2B/NMDA antagonist ; Molecular modeling ; Anticonvulsant activity ; Patch cl Binding affinity
- 刊名：Bioorganic and Medicinal Chemistry
- 出版年：2009
- 出版时间：15 February 2009
- 年：2009
- 卷：17
- 期：4
- 页码：1640-1647
- 全文大小：884 K
文摘
A combined ligand-based and structure-based approach has previously allowed us to identify NR2B/NMDA receptor antagonists containing indole scaffold. In order to further explore the main structure activity relationships of this class of derivatives we herein report the design, synthesis and biological evaluation of new analogues. Some derivatives demonstrated to produce significant anticonvulsant properties and NMDA antagonism. The most active of them (3d) showed NR2B binding affinity equipotent to that of ifenprodil. These results were also corroborated by computational studies.