Structure-activity relationships of 2,4-diphenyl-1H-imidazole analogs as CB2 receptor agonists for the treatment of chronic pain.
A series of 2,4-diphenyl-1H-imidazole analogs have been synthesized and displayed potent human CB2 agonist activity. Many of these analogs showed high functional selectivity over human CB1 receptors. The syntheses, structure-activity relationships, and selected pharmacokinetic data of these analogs are described.
Department of Chemical Research-CV & CNS, Merck Research Laboratory, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. shu-wei.yang@merck.com
Shu-Wei
SW
Yang
Jennifer
J
Smotryski
Julius
J
Matasi
Ginny
G
Ho
Deen
D
Tulshian
William J
WJ
Greenlee
Rossella
R
Brusa
Massimiliano
M
Beltramo
Kathleen
K
Cox
D000284:Administration, Oral; D000818:Animals; D002908:Chronic Disease; D006801:Humans; D007093:Imidazoles / Q000737:chemistry* / Q000493:pharmacokinetics / Q000627:therapeutic use; D010146:Pain / Q000188:drug therapy*; D051381:Rats; D043884:Receptor, Cannabinoid, CB1 / Q000819:agonists / Q000378:metabolism; D043885:Receptor, Cannabinoid, CB2 / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship
D007093:Imidazoles; D043884:Receptor, Cannabinoid, CB1; D043885:Receptor, Cannabinoid, CB2