2-Amino-5-aryl-pyridines as selective CB2 agonists: synthesis and investigation of structure-activity relationships.
2-Amino-5-aryl-pyridines, exemplified by compound 1, had been identified as a synthetically tractable series of CB(2) agonists from a high-throughput screen of the GlaxoSmithKline compound collection. Described herein are the results of an investigation of the structure-activity relationships (SAR) which led to the identification a number of potent and selective agonists.
Gleave
Robert J
RJ
Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex CM19 5AW, United Kingdom. robert.j.gleave@gsk.com
Beswick
Paul J
PJ
Brown
Andrew J
AJ
Giblin
Gerard M P
GM
Haslam
Carl P
CP
Livermore
David
D
Moses
Andrew
A
Nicholson
Neville H
NH
Page
Lee W
LW
Slingsby
Brian
B
Swarbrick
Martin E
ME
D015195:Drug Design; D015394:Molecular Structure; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D043885:Receptor, Cannabinoid, CB2 / Q000819:agonists*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D011725:Pyridines; D043885:Receptor, Cannabinoid, CB2