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

I Sellitto, B Le Bourdonnec, K Worm, A Goodman…

Index: Sellitto, Ian; Bourdonnec, Bertrand Le; 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. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 1 p. 387 - 391

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Citation Number: 11

Abstract

A lead optimization campaign in our previously reported sulfamoyl benzamide class of CB2 agonists was conducted to improve the in vitro metabolic stability profile in this series while retaining high potency and selectivity for the CB2 receptor. From this study, compound 14, N- (3, 4-dimethyl-5-(morpholinosulfonyl) phenyl)-2, 2-dimethylbutanamide, was identified as a potent and selective CB2 agonist exhibiting moderate in vitro metabolic stability and oral ...