Diaryl piperidines as CB1 receptor antagonists.

Scott, Jack D; Li, Sarah W; Wang, Hongwu; Xia, Yan; Jayne, Charles L; Miller, Michael W; Duffy, Ruth A; Boykow, George C; Kowalski, Timothy J; Spar, Brian D; Stamford, Andrew W; Chackalamannil, Samuel; Lachowicz, Jean E; Greenlee, William J

Scott, Jack D; Li, Sarah W; Wang, Hongwu; Xia, Yan; Jayne, Charles L; Miller, Michael W; Duffy, Ruth A; Boykow, George C; Kowalski, Timothy J; Spar, Brian D; Stamford, Andrew W; Chackalamannil, Samuel; Lachowicz, Jean E; Greenlee, William J.

Afiliación

Scott JD; Department of Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. jack.scott@spcorp.com

Bioorg Med Chem Lett ; 20(3): 1278-83, 2010 Feb 01.

Article en En | MEDLINE | ID: mdl-20018510

ABSTRACT

ABSTRACT

The syntheses and SAR investigations of novel CB(1) receptor antagonists based on a 1,2-diaryl piperidine core have been described. Optimization of this core afforded a compound with robust in vivo potency by reducing food intake in a mouse DIO model.

Asunto(s)

Piperidinas/química; Piperidinas/farmacología; Receptor Cannabinoide CB1/antagonistas & inhibidores; Animales; Dieta/efectos adversos; Ingestión de Alimentos/efectos de los fármacos; Ingestión de Alimentos/fisiología; Ratones; Ratones Obesos; Obesidad/etiología; Obesidad/metabolismo; Piperidinas/administración & dosificación; Unión Proteica/fisiología; Receptor Cannabinoide CB1/metabolismo; Relación Estructura-Actividad

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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Piperidinas / Receptor Cannabinoide CB1 Tipo de estudio: Etiology_studies Límite: Animals Idioma: En Año: 2010 Tipo del documento: Article

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