The discovery and synthesis of highly potent, A2a receptor agonists.
A series of N6,2-disubstituted adenosine analogues have been synthesized and their functional activity measured against A2a and A1 receptors. Examples of compounds with both a lipophilic N6-substituent and amino-functionalized 2-position were highly active at the A2a receptor on the human neutrophil.
Keeling
S E
SE
Medicinal Sciences, Glaxo Wellcome Medicines Research Centre, Stevenage, Herts, UK. ser0079@glaxowellcome.co.uk
Albinson
F D
FD
Ayres
B E
BE
Butchers
P R
PR
Chambers
C L
CL
Cherry
P C
PC
Ellis
F
F
Ewan
G B
GB
Gregson
M
M
Knight
J
J
Mills
K
K
Ravenscroft
P
P
Reynolds
L H
LH
Sanjar
S
S
Sheehan
M J
MJ
D000241:Adenosine / Q000031:analogs & derivatives / Q000737:chemistry* / Q000494:pharmacology*; D000893:Anti-Inflammatory Agents / Q000737:chemistry; D019204:GTP-Binding Proteins; D058906:Purinergic P1 Receptor Agonists; D012995:Solubility; D013329:Structure-Activity Relationship
D000893:Anti-Inflammatory Agents; D058906:Purinergic P1 Receptor Agonists; D019204:GTP-Binding Proteins; D000241:Adenosine