Enaminone amides as novel orally active GABAA receptor modulators

…, JC Huang, WY Li, M Tran, ER Whittemore…

文献索引：Hogenkamp, Derk J.; Johnstone, Timothy B. C.; Huang, Jin-Cheng; Li, Wen-Yen; Tran, Minhtam; Whittemore, Edward R.; Bagnera, Rudy E.; Gee, Kelvin W. Journal of Medicinal Chemistry, 2007 , vol. 50, # 14 p. 3369 - 3379

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被引用次数: 30

摘要

A series of enaminone esters and amides have been developed as potent allosteric modulators of γ-aminobutyric acidA (GABAA) receptors. The compounds bind to a novel modulatory site that is independent of the benzodiazepine (BZ), isosteric GABA, and neuroactive steroid binding sites. Structure-activity relationship (SAR) studies resulted in the synthesis of the c-Bu amide 16h with an in vitro potency of 7 nM based on inhibition of [ ...