Synthesis and SAR of 5-, 6-, 7-and 8-aza analogues of 3-aryl-4-hydroxyquinolin-2 (1H)-one as NMDA/glycine site antagonists

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

Index: Zhou, Zhang-Lin; Navratil, James 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, 2001 , vol. 9, # 8 p. 2061 - 2071

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Citation Number: 32

Abstract

A series of 5-, 6-, 7-and 8-aza analogues of 3-aryl-4-hydroxyquinolin-2 (1H)-one was synthesized and assayed as NMDA/glycine receptor antagonists. The in vitro potency of these antagonists was determined by displacement of the glycine site radioligand [3H] 5, 7- dicholorokynurenic acid ([3H] DCKA) in rat brain cortical membranes. Selected compounds were also tested for functional antagonism using electrophysiological assays in Xenopus ...