CB2 selective sulfamoyl benzamides: Optimization of the amide functionality
| Autor: | Bertrand Le Bourdonnec, Patrick J. Little, Christopher W. Ajello, Bernice L. Brogdon, Markku A. Savolainen, Steven A. Smith, Michael Koblish, Allan J. Goodman, Christopher J. LaBuda, Robert N. DeHaven, Heather O’Hare, Roland E. Dolle, Joel A. Cassel, Karin Worm, Gabriel J. Stabley |
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| Rok vydání: | 2009 |
| Předmět: |
Cannabinoid receptor
Stereochemistry medicine.medical_treatment Clinical Biochemistry Pain Pharmaceutical Science Rodentia Pharmacology Biochemistry Receptor Cannabinoid CB2 chemistry.chemical_compound Oral administration Amide Drug Discovery medicine Animals Receptor Molecular Biology biology Chemistry Organic Chemistry Cytochrome P450 Benzamides biology.protein Molecular Medicine Cannabinoid |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 19:309-313 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2008.11.091 |
| Popis: | Previous research within our laboratories identified sulfamoyl benzamides as novel cannabinoid receptor ligands. Optimization of the amide linkage led to the reverse amide 40. The compound exhibited robust antiallodynic activity in a rodent pain model when administered intraperitoneally. Efficacy after oral administration was observed only when ABT, a cytochrome P450 suicide inhibitor, was coadministered. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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