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...

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Published inBioorganic & medicinal chemistry letters Vol. 10; no. 4; pp. 403 - 406
Main Authors KEELING, S. E, ALBINSON, F. D, MILLS, K, RAVENSCROFT, P, REYNOLDS, L. H, SANJAR, S, SHEEHAN, M. J, AYRES, B. E, BUTCHERS, P. R, CHAMBERS, C. L, CHERRY, P. C, ELLIS, F, EWAN, G. B, GREGSON, M, KNIGHT, J
Format Journal Article
LanguageEnglish
Published Oxford Elsevier 21.02.2000
Subjects
Adenosine - analogs & derivatives
Adenosine - chemistry
Adenosine - pharmacology
Anti-Inflammatory Agents - chemistry
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
GTP-Binding Proteins
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
Purinergic P1 Receptor Agonists
Solubility
Structure-Activity Relationship
Human
Agonist
Purine nucleoside
Solubility
In vitro
A2 Adenosine receptor
Amine
Structure activity relation
Uronic acid
Organic amide
Neutrophil
Chemical synthesis
Physicochemical properties
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Summary: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.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
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ISSN:0960-894X
1464-3405