Discovery of α-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.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009, Vol.19 (1), p.31-35
Hauptverfasser:	MARX, Isaac E, DIMAURO, Erin F, MARTIN, Matthew W, WHITE, Ryan D, FREMEAU, Robert T, PATEL, Vinod F, CHENG, Alan, EMKEY, Renee, HITCHCOCK, Stephen A, LIYUE HUANG, HUANG, Ming Y, HUMAN, Jason, LEE, Josie H, XINGWEN LI
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemistry Amides - pharmacology Animals Biological and medical sciences Humans Medical sciences Microsomes, Liver Miscellaneous Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacokinetics Pharmacology. Drug treatments Rats Receptor, Cannabinoid, CB2 - agonists Structure-Activity Relationship Sulfones - chemistry Sulfones - pharmacology
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Beschreibung
Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2008.11.026