Diaryl piperidines as CB1 receptor antagonists.
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Scott JD, Li SW, Wang H, Xia Y, Jayne CL, Miller MW, Duffy RA, Boykow GC, Kowalski TJ, Spar BD, Stamford AW, Chackalamannil S, Lachowicz JE, Greenlee WJ
Diaryl piperidines as CB1 receptor antagonists.
Bioorg Med Chem Lett. 2010 Feb 1;20(3):1278-83. doi: 10.1016/j.bmcl.2009.11.075. Epub 2009 Nov 20.
- PubMed ID
- 20018510 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Rimonabant Cannabinoid receptor 1 Ki (nM) 2.4 N/A N/A Details