Selective NR1/2B N-methyl-D-aspartate receptor antagonists among indole-2-carboxamides and benzimidazole-2-carboxamides

I Borza, E Bozo, G Barta-Szalai, C Kiss…

Index: Borza, Istvan; Bozo, Eva; Barta-Szalai, Gizella; Kiss, Csilla; Tarkanyi, Gabor; Demeter, Adam; Gati, Tamas; Hada, Viktor; Kolok, Sandor; Gere, Aniko; Fodor, Laszlo; Nagy, Jozsef; Galgoczy, Kornel; Magdo, Ildiko; Agai, Bela; Fetter, Jozsef; Bertha, Ferenc; Keserue, Gyoergy M.; Horvath, Csilla; Farkas, Sandor; Greiner, Istvan; Domany, Gyoergy Journal of Medicinal Chemistry, 2007 , vol. 50, # 5 p. 901 - 914

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Citation Number: 35

Abstract

(4-Benzylpiperidine-1-yl)-(6-hydroxy-1 H-indole-2-yl)-methanone (6a) derived from (E)-1-(4- benzylpiperidin-1-yl)-3-(4-hydroxy-phenyl)-propenone (5) was identified as a potent NR2B subunit-selective antagonist of the NMDA receptor. To establish the structure-activity relationship (SAR) and to attempt the improvement of the ADME properties of the lead, a series of compounds were prepared and tested. Several derivatives showed low ...