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Sulfamoyl benzamides as novel CB2 cannabinoid receptor ligands
Authors:Worm Karin  Zhou Q Jean  Saeui Christopher T  Green Rosalyn C  Cassel Joel A  Stabley Gabriel J  DeHaven Robert N  Conway-James Nathalie  LaBuda Christopher J  Koblish Michael  Little Patrick J  Dolle Roland E
Affiliation:

aDepartment of Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA, USA

bDepartment of Pharmacology, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA, USA

Abstract:Sulfamoyl benzamides were identified as a novel series of cannabinoid receptor ligands. Starting from a screening hit 8 that had modest affinity for the cannabinoid CB2 receptor, a parallel synthesis approach and initial SAR are described, leading to compound 27 with 120-fold functional selectivity for the CB2 receptor. This compound produced robust antiallodynic activity in rodent models of postoperative pain and neuropathic pain without traditional cannabinergic side effects.
Keywords:Cannabinoid CB2 receptor   Parallel synthesis   Sulfamoyl benzamides   Structure–activity relationship   Antiallodynic activity
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