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.

Affiliation

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 in 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.

Subject(s)

Piperidines/chemistry; Piperidines/pharmacology; Receptor, Cannabinoid, CB1/antagonists & inhibitors; Animals; Diet/adverse effects; Eating/drug effects; Eating/physiology; Mice; Mice, Obese; Obesity/etiology; Obesity/metabolism; Piperidines/administration & dosage; Protein Binding/physiology; Receptor, Cannabinoid, CB1/metabolism; Structure-Activity Relationship

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Piperidines / Receptor, Cannabinoid, CB1 Type of study: Etiology_studies Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2010 Document type: Article Affiliation country: United States

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