CB2 selective sulfamoyl benzamides: optimization of the amide functionality.

Bioorg Med Chem Lett 2009 Jan 27;19(2):309-13. Epub 2008 Nov 27.

Department of Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA.

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.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2008.11.091DOI Listing
January 2009
15 Reads
2.420 Impact Factor

Publication Analysis

Top Keywords

optimization amide
8
sulfamoyl benzamides
8
led reverse
4
reverse amide
4
administration observed
4
amide compound
4
observed abt
4
linkage led
4
administered intraperitoneally
4
ligands optimization
4
abt cytochrome
4
amide linkage
4
compound exhibited
4
oral administration
4
rodent pain
4
intraperitoneally efficacy
4
pain model
4
model administered
4
activity rodent
4
efficacy oral
4

Similar Publications