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. 2010 Jan 1;20(1):387-91.
doi: 10.1016/j.bmcl.2009.10.062. Epub 2009 Oct 17.

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

Ian Sellitto  1 , Bertrand Le Bourdonnec, Karin Worm, Allan Goodman, Markku A Savolainen, Guo-Hua Chu, Christopher W Ajello, Christopher T Saeui, Lara K Leister, Joel A Cassel, Robert N Dehaven, Christopher J Labuda, Michael Koblish, Patrick J Little, Bernice L Brogdon, Steven A Smith, Roland E Dolle
Affiliations

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

Ian Sellitto et al. Bioorg Med Chem Lett. .

Abstract

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

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