title: CB2 selective sulfamoyl benzamides: optimization of the amide functionality.
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.
authors.affiliation: Department of Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA. agoodman@adolor.com
authors.forename: Allan J
authors.initials: AJ
authors.lastname: Goodman
authors.forename: Christopher W
authors.initials: CW
authors.lastname: Ajello
authors.forename: Karin
authors.initials: K
authors.lastname: Worm
authors.forename: Bertrand
authors.initials: B
authors.lastname: Le Bourdonnec
authors.forename: Markku A
authors.initials: MA
authors.lastname: Savolainen
authors.forename: Heather
authors.initials: H
authors.lastname: O'Hare
authors.forename: Joel A
authors.initials: JA
authors.lastname: Cassel
authors.forename: Gabriel J
authors.initials: GJ
authors.lastname: Stabley
authors.forename: Robert N
authors.initials: RN
authors.lastname: Dehaven
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Labuda
authors.forename: Michael
authors.initials: M
authors.lastname: Koblish
authors.forename: Patrick J
authors.initials: PJ
authors.lastname: Little
authors.forename: Bernice L
authors.initials: BL
authors.lastname: Brogdon
authors.forename: Steven A
authors.initials: SA
authors.lastname: Smith
authors.forename: Roland E
authors.initials: RE
authors.lastname: Dolle
mesh_terms: 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
chemical_list: D001549:Benzamides; D043885:Receptor, Cannabinoid, CB2