Tricyclic indole-2-carboxylic acids: highly in vivo active and selective antagonists for the glycine binding site of the NMDA receptor

S Katayama, N Ae, T Kodo, S Masumoto…

文献索引：Katayama, Seiji; Ae, Nobuyuki; Kodo, Toru; Masumoto, Shuji; Hourai, Shinji; Tamamura, Chika; Tanaka, Hiroyasu; Nagata, Ryu Journal of Medicinal Chemistry, 2003 , vol. 46, # 5 p. 691 - 701

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被引用次数: 30

摘要

A series of tricyclic indole-2-carboxylic acid derivatives were synthesized and evaluated by the radioligand binding assay and the anticonvulsant effects in the mouse NMDA-induced seizure model. Among them, derivatives of 3 S-(-)-4 such as 3a, 3f, and 3g which had certain zwitterionic anilides showed high affinity to the NMDA-glycine binding site. The absolute configuration of 3 S-(-)-4 was confirmed by X-ray crystallographic analysis. In particular, ...