2-Carboxytetrahydroquinolines. Conformational and stereochemical requirements for antagonism of the glycine site on the N-methyl-D-aspartate (NMDA) receptor

RW Carling, PD Leeson, AM Moseley…

Index: Carling, Robert W.; Leeson, Paul D.; Moseley, Angela M.; Baker, Raymond; Foster, Alan C.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 11 p. 1942 - 1953

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Citation Number: 100

Abstract

P-Car~ xy-l, 2, 3, 4-tetrahydroquo~ e derivatives, derived from kynurenic acid, have been synthesized and evaluated for in vitro antagonist activity at the glycine site on the NMDA receptor. 2, 3-Dihydrokynurenic acids show reduced potency relative to the parent lead compounds (Table I) possibly as a result of conformational effects. Removal of the 40x0 group results in further reduced potency, but introduction of a cis-carboxymethyl group to ...