title: Triaryl bis-sulfones as cannabinoid-2 receptor ligands: SAR studies.
abstract: 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.
authors.affiliation: Department of Chemistry, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033-0539, USA. bandarpalle.shankar@spcorp.com
authors.forename: Bandarpalle B
authors.initials: BB
authors.lastname: Shankar
authors.forename: Brian J
authors.initials: BJ
authors.lastname: Lavey
authors.forename: Guowei
authors.initials: G
authors.lastname: Zhou
authors.forename: James A
authors.initials: JA
authors.lastname: Spitler
authors.forename: Ling
authors.initials: L
authors.lastname: Tong
authors.forename: Razia
authors.initials: R
authors.lastname: Rizvi
authors.forename: De-Yi
authors.initials: DY
authors.lastname: Yang
authors.forename: Ronald
authors.initials: R
authors.lastname: Wolin
authors.forename: Joseph A
authors.initials: JA
authors.lastname: Kozlowski
authors.forename: Neng-Yang
authors.initials: NY
authors.lastname: Shih
authors.forename: Jie
authors.initials: J
authors.lastname: Wu
authors.forename: R William
authors.initials: RW
authors.lastname: Hipkin
authors.forename: Waldemar
authors.initials: W
authors.lastname: Gonsiorek
authors.forename: Charles A
authors.initials: CA
authors.lastname: Lunn
mesh_terms: D008024:Ligands; D043885:Receptor, Cannabinoid, CB2 / Q000037:antagonists & inhibitors / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology
chemical_list: D008024:Ligands; D043885:Receptor, Cannabinoid, CB2; D013450:Sulfones