3-Hydroxy-quinolin-2-ones: Inhibitors of [3 H]-glycine binding to the site associated with the NMDA receptor

SY Sit, FJ Ehrgott, J Gao, NA Meanwell

Index: Sit, Sing-Yuen; Ehrgott, Frederick J.; Gao, Jinnian; Meanwell, Nicholas A. Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 5 p. 499 - 504

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Citation Number: 17

Abstract

A series of substituted 3-hydroxy-quinolin-2-one derivatives 6 was synthesized and evaluated as inhibitors of [3H]-glycine and [3H]-AMPA binding to rat cortical membranes. These compounds were generally found to be more potent ligands for the NMDA-associated glycine binding site than the AMPA receptor. Affinity for the glycine site was found to be influenced by both the electronic and steric properties associated with the C-4 substitutent ...