Details

Autor(en) / Beteiligte

• Sellitto, Ian
• Le Bourdonnec, Bertrand
• Worm, Karin
• Goodman, Allan
• Savolainen, Markku A
• Chu, Guo-Hua
• Ajello, Christopher W
• Saeui, Christopher T
• Leister, Lara K
• Cassel, Joel A
• DeHaven, Robert N
• LaBuda, Christopher J
• Koblish, Michael
• Little, Patrick J
• Brogdon, Bernice L
• Smith, Steven A
• Dolle, Roland E

Titel

Novel sulfamoyl benzamides as selective CB sub(2) agonists with improved in vitro metabolic stability

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2010-01, Vol.20 (1), p.387-391

Erscheinungsjahr

2010

Link zum Volltext

Quelle

Elsevier ScienceDirect Journals Complete

Beschreibungen/Notizen

• A lead optimization campaign in our previously reported sulfamoyl benzamide class of CB sub(2) agonists was conducted to improve the in vitro metabolic stability profile in this series while retaining high potency and selectivity for the CB sub(2) receptor. From this study, compound 14, N-(3,4-dimethyl-5-(morpholinosulfonyl)phenyl)-2,2-dimethylbutan amide, was identified as a potent and selective CB sub(2) agonist exhibiting moderate in vitro metabolic stability and oral bioavailability. Compound 14 demonstrated in vivo efficacy in a rat model of post-surgical pain.