CB2 selective sulfamoyl benzamides: Optimization of the amide functionality

Allan J. Goodman, Christopher W. Ajello, Karin Worm, Bertrand Le Bourdonnec, Markku A. Savolainen, Heather O'Hare, Joel A. Cassel, Gabriel J. Stabley, Robert N. DeHaven, Christopher J. LaBuda, Michael Koblish, Patrick J. Little, Bernice L. Brogdon, Steven A. Smith, Roland E. Dolle

Research output: Contribution to journalArticle

18 Scopus citations

Abstract

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.

Original languageEnglish
Pages (from-to)309-313
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number2
DOIs
StatePublished - Jan 15 2009
Externally publishedYes

Keywords

  • Antiallodynia
  • CB1
  • CB2
  • Cannabinoid
  • Sulfamoyl benzamides

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    Goodman, A. J., Ajello, C. W., Worm, K., Bourdonnec, B. L., Savolainen, M. A., O'Hare, H., Cassel, J. A., Stabley, G. J., DeHaven, R. N., LaBuda, C. J., Koblish, M., Little, P. J., Brogdon, B. L., Smith, S. A., & Dolle, R. E. (2009). CB2 selective sulfamoyl benzamides: Optimization of the amide functionality. Bioorganic and Medicinal Chemistry Letters, 19(2), 309-313. https://doi.org/10.1016/j.bmcl.2008.11.091