The discovery of novel indole-2-carboxamides as cannabinoid CB(1) receptor antagonists.

Cowley, Phillip M; Baker, James; Barn, David R; Buchanan, Kirsteen I; Carlyle, Ian; Clark, John K; Clarkson, Thomas R; Deehan, Maureen; Edwards, Darren; Goodwin, Richard R; Jaap, David; Kiyoi, Yasuko; Mort, Chris; Palin, Ronald; Prosser, Alan; Walker, Glenn; Ward, Nick; Wishart, Grant; Young, Trevor

Cowley, Phillip M; Baker, James; Barn, David R; Buchanan, Kirsteen I; Carlyle, Ian; Clark, John K; Clarkson, Thomas R; Deehan, Maureen; Edwards, Darren; Goodwin, Richard R; Jaap, David; Kiyoi, Yasuko; Mort, Chris; Palin, Ronald; Prosser, Alan; Walker, Glenn; Ward, Nick; Wishart, Grant; Young, Trevor.

Afiliación

Cowley PM; Department of Chemistry, MSD, Newhouse, Lanarkshire ML1 5SH, UK. phillip.cowley@merck.com

Bioorg Med Chem Lett ; 21(1): 497-501, 2011 Jan 01.

Article en En | MEDLINE | ID: mdl-21075628

RESUMEN

The discovery and structure-activity relationship of a novel series of indole-2-carboxamide antagonists of the cannabinoid CB(1) receptor is disclosed. Compound 26i was found to be a high potency, selective cannabinoid CB(1) antagonist.

Asunto(s)

Amidas/química; Indoles/química; Receptor Cannabinoide CB1/antagonistas & inhibidores; Amidas/síntesis química; Amidas/farmacocinética; Animales; Perros; Evaluación Preclínica de Medicamentos; Indoles/síntesis química; Indoles/farmacocinética; Masculino; Ratones; Modelos Moleculares; Ratas; Ratas Wistar; Receptor Cannabinoide CB1/metabolismo; Relación Estructura-Actividad

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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptor Cannabinoide CB1 / Amidas / Indoles Límite: Animals Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2011 Tipo del documento: Article Pais de publicación: Reino Unido

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