Discovery of alpha-amidosulfones as potent and selective agonists of CB2: synthesis, SAR, and pharmacokinetic properties.
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.
Marx
Isaac E
IE
Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Cambridge, MA 02139, USA. imarx@amgen.com
DiMauro
Erin F
EF
Cheng
Alan
A
Emkey
Renee
R
Hitchcock
Stephen A
SA
Huang
Liyue
L
Huang
Ming Y
MY
Human
Jason
J
Lee
Josie H
JH
Li
Xingwen
X
Martin
Matthew W
MW
White
Ryan D
RD
Fremeau
Robert T
RT
Patel
Vinod F
VF
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
D000577:Amides; D043885:Receptor, Cannabinoid, CB2; D013450:Sulfones