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.
Goodman
Allan J
AJ
Department of Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA. agoodman@adolor.com
Ajello
Christopher W
CW
Worm
Karin
K
Le Bourdonnec
Bertrand
B
Savolainen
Markku A
MA
O'Hare
Heather
H
Cassel
Joel A
JA
Stabley
Gabriel J
GJ
Dehaven
Robert N
RN
Labuda
Christopher J
CJ
Koblish
Michael
M
Little
Patrick J
PJ
Brogdon
Bernice L
BL
Smith
Steven A
SA
Dolle
Roland E
RE
D000818:Animals; D001549:Benzamides / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D010146:Pain / Q000188:drug therapy; D043885:Receptor, Cannabinoid, CB2 / Q000187:drug effects*; D012377:Rodentia
D001549:Benzamides; D043885:Receptor, Cannabinoid, CB2