The discovery and synthesis of highly potent, A2a receptor agonists

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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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2000-02, Vol.10 (4), p.403-406
Hauptverfasser: 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: Artikel
Sprache:eng
Schlagworte:
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
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Zusammenfassung: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.
ISSN:0960-894X
1464-3405