933474-60-3Relevant academic research and scientific papers
Selective NR1/2B N-methyl-D-aspartate receptor antagonists among indole-2-carboxamides and benzimidazole-2-carboxamides
Borza, István,Bozó, éva,Barta-Szalai, Gizella,Kiss, Csilla,Tárkányi, Gábor,Demeter, ádám,Gáti, Tamás,Háda, Viktor,Kolok, Sándor,Gere, Anikó,Fodor, László,Nagy, József,Galgóczy, Kornél,Magdó, Ildikó,ágai, Béla,Fetter, József,Bertha, Ferenc,Keserü, Gy?rgy M.,Horváth, Csilla,Farkas, Sándor,Greiner, István,Domány, Gy?rgy
, p. 901 - 914 (2008/02/03)
(4-Benzylpiperidine-1-yl)-(6-hydroxy-1H-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 structu
Amide derivatives as NMDA receptor antagonists
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, (2008/06/13)
New Formula (I) compounds are disclosed having NR2B selective NMDA receptor antagonist activity wherein one of the neighboring R1, R2, R3 and R4 groups is OH or NH2 and the others are each hydrogen , or two of the neighboring R1, R2 R3 and R4 groups in given case together with one or more identical or different additional hetero atom and —CH═ and/or —CH2— groups forms a 5-6 membered homo- or heterocyclic ring, preferably pyrrole, pyrazole, imidazole, oxazole, oxo-oxazolidine, or 3-oxo-1,4-oxazine ring, and the other two of R1, R2, R3 and R4 groups are is hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by hydroxy group, and/or in given case phenyl or phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), anilino, phenyl-(C1-C4 alkylamino), [phenyl-(C1-C4 alkyl)]-amino, benzoyl, hydroxy-diphenylmethyl, C1-C4 alkoxycarbonyl-phenoxymethyl or benzhydrylidene group, optionally substituted on the aromatic ring by one or more halogen atom, cyano or hydroxy group, C1-C4 alkyl or C1-C4 alkoxy group, X is independently oxygen, —NH— or a CH2 group, Y is independently a nitrogen atom or a —CH— group, and the salts thereof formed with acids and bases.
