The discovery and synthesis of highly potent, A2a receptor agonists

S E Keeling; F D Albinson; B E Ayres; P R Butchers; C L Chambers; P C Cherry; F Ellis; G B Ewan; M Gregson; J Knight; K Mills; P Ravenscroft; L H Reynolds; S Sanjar; M J Sheehan

doi:10.1016/s0960-894x(00)00017-2

The discovery and synthesis of highly potent, A2a receptor agonists

Bioorg Med Chem Lett. 2000 Feb 21;10(4):403-6. doi: 10.1016/s0960-894x(00)00017-2.

Authors

S E Keeling¹, F D Albinson, B E Ayres, P R Butchers, C L Chambers, P C Cherry, F Ellis, G B Ewan, M Gregson, J Knight, K Mills, P Ravenscroft, L H Reynolds, S Sanjar, M J Sheehan

Affiliation

¹ Medicinal Sciences, Glaxo Wellcome Medicines Research Centre, Stevenage, Herts, UK. ser0079@glaxowellcome.co.uk

PMID: 10714510
DOI: 10.1016/s0960-894x(00)00017-2

Abstract

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.

MeSH terms

Adenosine / analogs & derivatives
Adenosine / chemistry*
Adenosine / pharmacology*
Anti-Inflammatory Agents / chemistry
GTP-Binding Proteins
Purinergic P1 Receptor Agonists*
Solubility
Structure-Activity Relationship

Substances

Anti-Inflammatory Agents
Purinergic P1 Receptor Agonists
GTP-Binding Proteins
Adenosine