Discovery of alpha-amidosulfones as potent and selective agonists of CB2: synthesis, SAR, and pharmacokinetic properties

Isaac E Marx; Erin F DiMauro; Alan Cheng; Renee Emkey; Stephen A Hitchcock; Liyue Huang; Ming Y Huang; Jason Human; Josie H Lee; Xingwen Li; Matthew W Martin; Ryan D White; Robert T Fremeau Jr; Vinod F Patel

doi:10.1016/j.bmcl.2008.11.026

Discovery of alpha-amidosulfones as potent and selective agonists of CB2: synthesis, SAR, and pharmacokinetic properties

Bioorg Med Chem Lett. 2009 Jan 1;19(1):31-5. doi: 10.1016/j.bmcl.2008.11.026. Epub 2008 Nov 13.

Authors

Isaac E Marx¹, Erin F DiMauro, Alan Cheng, Renee Emkey, Stephen A Hitchcock, Liyue Huang, Ming Y Huang, Jason Human, Josie H Lee, Xingwen Li, Matthew W Martin, Ryan D White, Robert T Fremeau Jr, Vinod F Patel

Affiliation

¹ Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Cambridge, MA 02139, USA. imarx@amgen.com

PMID: 19062274
DOI: 10.1016/j.bmcl.2008.11.026

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.

MeSH terms

Amides / chemistry
Amides / pharmacology
Animals
Humans
Microsomes, Liver
Pharmacokinetics
Rats
Receptor, Cannabinoid, CB2 / agonists*
Structure-Activity Relationship
Sulfones / chemistry*
Sulfones / pharmacology

Substances

Amides
Receptor, Cannabinoid, CB2
Sulfones