Triaryl bis-sulfones as cannabinoid-2 receptor ligands: SAR studies.
We recently reported that compound 1 is a potent inhibitor of the CB2 receptor with high selectivity over CB1. This paper describes the SAR development for this class of compounds. Variation of the substitution pattern on the aromatic rings, as well as the groups linking them together, led to sub-nanomolar inhibitors of the CB2 receptor, with high selectivity over CB1.
Shankar
Bandarpalle B
BB
Department of Chemistry, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033-0539, USA. bandarpalle.shankar@spcorp.com
Lavey
Brian J
BJ
Zhou
Guowei
G
Spitler
James A
JA
Tong
Ling
L
Rizvi
Razia
R
Yang
De-Yi
DY
Wolin
Ronald
R
Kozlowski
Joseph A
JA
Shih
Neng-Yang
NY
Wu
Jie
J
Hipkin
R William
RW
Gonsiorek
Waldemar
W
Lunn
Charles A
CA
D008024:Ligands; D043885:Receptor, Cannabinoid, CB2 / Q000037:antagonists & inhibitors / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology
D008024:Ligands; D043885:Receptor, Cannabinoid, CB2; D013450:Sulfones