Abstract
Structure-activity relationships and efforts to optimize the pharmacokinetic profile of isosteric analogs of 2-arylimino-5,6-dihydro-4H-1,3-thiazines as cannabinoid receptor agonists are described. Among those examined, compound 25 showed potent affinity for cannabinoid receptor 1 (CB1) and receptor 2 (CB2). This compound displayed oral bioavailability and analgesic activity.
MeSH terms
-
Administration, Oral
-
Animals
-
Biological Availability
-
Cannabinoid Receptor Agonists*
-
Cell Line, Tumor
-
Chemistry, Pharmaceutical / methods
-
Drug Design
-
Humans
-
Kinetics
-
Mice
-
Models, Chemical
-
Rats
-
Structure-Activity Relationship
-
Thiazines / chemical synthesis*
-
Thiazines / pharmacokinetics
-
Thiazines / pharmacology*
-
Thiourea / chemistry
Substances
-
Cannabinoid Receptor Agonists
-
Thiazines
-
Thiourea