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.
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
Robert J
RJ
Gleave
Paul J
PJ
Beswick
Andrew J
AJ
Brown
Gerard M P
GM
Giblin
Carl P
CP
Haslam
David
D
Livermore
Andrew
A
Moses
Neville H
NH
Nicholson
Lee W
LW
Page
Brian
B
Slingsby
Martin E
ME
Swarbrick
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