Substituted indole-2-carboxylates as in vivo potent antagonists acting as the strychnine-insensitive glycine binding site

…, M Mugnaini, A Pecunioso, AM Quaglia…

Index: Di Fabio, Romano; Capelli, Anna M.; Conti, Nadia; Cugola, Alfredo; Donati, Daniele; Feriani, Aldo; Gastaldi, Paola; Gaviraghi, Giovanni; Hewkin, Cheryl T.; Micheli, Fabrizio; Missio, Andrea; Mugnaini, Manolo; Pecunioso, Angelo; Quaglia, Anna M.; Ratti, Emiliangelo; Rossi, Luciana; Tedesco, Giovanna; Trist, David G.; Reggiani, Angelo Journal of Medicinal Chemistry, 1997 , vol. 40, # 6 p. 841 - 850

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Citation Number: 93

Abstract

A series of indole-2-carboxylates bearing suitable chains at the C-3 position of the indole nucleus was synthesized and evaluated in terms of in vitro affinity using [3H] glycine binding assay and in vivo potency by inhibition of convulsions induced by N-methyl-d-aspartate (NMDA) in mice. 3-[2-[(Phenylamino) carbonyl] ethenyl]-4, 6-dichloroindole-2-carboxylic acid (8) was an antagonist at the strychnine-insensitive glycine binding site ( ...