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ID: ALA1152695

Journal: Bioorg Med Chem

Title: Development of 3-substituted-1H-indole derivatives as NR2B/NMDA receptor antagonists.

Authors: Gitto R, De Luca L, Ferro S, Citraro R, De Sarro G, Costa L, Ciranna L, Chimirri A.

Abstract: 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.

CiteXplore: 19157884

DOI: 10.1016/j.bmc.2008.12.058