TY - JOUR
T1 - Sulfamoyl benzamides as novel CB2 cannabinoid receptor ligands
AU - Worm, Karin
AU - Zhou, Q. Jean
AU - Saeui, Christopher T.
AU - Green, Rosalyn C.
AU - Cassel, Joel A.
AU - Stabley, Gabriel J.
AU - DeHaven, Robert N.
AU - Conway-James, Nathalie
AU - LaBuda, Christopher J.
AU - Koblish, Michael
AU - Little, Patrick J.
AU - Dolle, Roland E.
PY - 2008/5/1
Y1 - 2008/5/1
N2 - 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.
AB - 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.
KW - Antiallodynic activity
KW - Cannabinoid CB receptor
KW - Parallel synthesis
KW - Structure-activity relationship
KW - Sulfamoyl benzamides
UR - http://www.scopus.com/inward/record.url?scp=43049150442&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2008.04.006
DO - 10.1016/j.bmcl.2008.04.006
M3 - Article
C2 - 18430570
AN - SCOPUS:43049150442
SN - 0960-894X
VL - 18
SP - 2830
EP - 2835
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 9
ER -