Novel N1-(benzyl)cinnamamidine derived NR2B subtype-selective NMDA receptor antagonists.

Curtis, Neil R; Diggle, Helen J; Kulagowski, Janusz J; London, Clare; Grimwood, Sarah; Hutson, Peter H; Murray, Fraser; Richards, Pawel; Macaulay, Alison; Wafford, Keith A

Curtis, Neil R; Diggle, Helen J; Kulagowski, Janusz J; London, Clare; Grimwood, Sarah; Hutson, Peter H; Murray, Fraser; Richards, Pawel; Macaulay, Alison; Wafford, Keith A.

Afiliación

Curtis NR; Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK. neil_curtis@merck.com

Bioorg Med Chem Lett ; 13(4): 693-6, 2003 Feb 24.

Article en En | MEDLINE | ID: mdl-12639560

ABSTRACT

ABSTRACT

Novel (E)-N(1)-(benzyl)cinnamamidines were prepared and evaluated as NR2B subtype NMDA receptor ligands. Excellent affinity was achieved by appropriate substitution of either phenyl ring. The 2-methoxybenzyl compound 1h had approximately 1,000-fold lower IC(50) in NR2B than NR2A-containing cells. Replacement of the styryl unit by 2-naphthyl was well tolerated.

Asunto(s)

Amidinas/síntesis química; Receptores de N-Metil-D-Aspartato/antagonistas & inhibidores; Amidinas/metabolismo; Benzamidinas/síntesis química; Benzamidinas/metabolismo; Evaluación Preclínica de Medicamentos; Humanos; Naftalenos/síntesis química; Naftalenos/metabolismo; Unión Proteica; Ensayo de Unión Radioligante; Receptores de N-Metil-D-Aspartato/metabolismo; Relación Estructura-Actividad

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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptores de N-Metil-D-Aspartato / Amidinas Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2003 Tipo del documento: Article País de afiliación: Reino Unido

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