title: Discovery of alpha-amidosulfones as potent and selective agonists of CB2: synthesis, SAR, and pharmacokinetic properties.
abstract: A series of alpha-amidosulfones were found to be potent and selective agonists of CB(2). The discovery, synthesis, and structure-activity relationships of this series of agonists are reported. In addition, the pharmacokinetic properties of the most promising compounds are profiled.
authors.affiliation: Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Cambridge, MA 02139, USA. imarx@amgen.com
authors.forename: Isaac E
authors.initials: IE
authors.lastname: Marx
authors.forename: Erin F
authors.initials: EF
authors.lastname: DiMauro
authors.forename: Alan
authors.initials: A
authors.lastname: Cheng
authors.forename: Renee
authors.initials: R
authors.lastname: Emkey
authors.forename: Stephen A
authors.initials: SA
authors.lastname: Hitchcock
authors.forename: Liyue
authors.initials: L
authors.lastname: Huang
authors.forename: Ming Y
authors.initials: MY
authors.lastname: Huang
authors.forename: Jason
authors.initials: J
authors.lastname: Human
authors.forename: Josie H
authors.initials: JH
authors.lastname: Lee
authors.forename: Xingwen
authors.initials: X
authors.lastname: Li
authors.forename: Matthew W
authors.initials: MW
authors.lastname: Martin
authors.forename: Ryan D
authors.initials: RD
authors.lastname: White
authors.forename: Robert T
authors.initials: RT
authors.lastname: Fremeau
authors.forename: Vinod F
authors.initials: VF
authors.lastname: Patel
mesh_terms: D000577:Amides / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D006801:Humans; D008862:Microsomes, Liver; D010599:Pharmacokinetics; D051381:Rats; D043885:Receptor, Cannabinoid, CB2 / Q000819:agonists*; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000577:Amides; D043885:Receptor, Cannabinoid, CB2; D013450:Sulfones