Atropisomeric quinazolin-4-one derivatives are potent noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists

…, K Kelly, PA Seymour, V Guanowsky, S Guhan…

文献索引：Welch; Ewing; Huang; Menniti; Pagnozzi; Kelly; Seymour; Guanowsky; Guhan; Guinn; Critchett; Lazzaro; Ganong; DeVries; Staigers; Chenard Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 2 p. 177 - 181

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被引用次数: 104

摘要

Piriqualone (1) was found to be an antagonist of AMPA receptors. Structure–activity optimization was conducted on each of the three rings in 1 to afford a series of potent and selective antagonists. The sterically crowded environment surrounding the N-3 aryl group provided sufficient thermal stability for atropisomers to be isolated. Separation of these atropisomers resulted in the identification of (+)-38 (CP-465,022), a compound that binds ...