CB2 selective sulfamoyl benzamides: Optimization of the amide functionality

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.

Isosteric replacement of the amide linkage was investigated. Reversal of the amide functionality led to a series of highly selective CB2 receptor agonists.Figure optionsDownload as PowerPoint slide