Synthesis and SAR of novel di-and trisubstituted 1, 4-dihydroquinoxaline-2, 3-diones related to licostinel (Acea 1021) as NMDA/glycine site antagonists

…, M Tran, RM Woodward, E Weber, JFW Keana

Index: Zhou, Zhang-Lin; Kher, Sunil M.; Cai, Sui Xiong; Whittemore, Edward R.; Espitia, Stephen A.; Hawkinson, Jon E.; Tran, Minhtam; Woodward, Richard M.; Weber, Eckard; Keana, John F. W. Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 8 p. 1769 - 1780

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Citation Number: 35

Abstract

A series of novel di-and trisubstituted 1, 4-dihydroquinoxaline-2, 3-diones (QXs) related to licostinel (Acea 1021) was synthesized and evaluated as antagonists for the glycine site of the N-methyl-d-asparate (NMDA) receptor. The in vitro potency of these antagonists was determined by displacement of the glycine site radioligand [3H]-5, 7-dichlorokynurenic acid ([3H] DCKA) in rat brain cortical membranes. Structure–activity relationship studies ...