Synthesis and evaluation of two series of 4′-aza-carbocyclic nucleosides as adenosine A2A receptor agonists

Beattie, David, Brearley, Andrew, Brown, Zarin, Charlton, Steven J, Cox, Brian, Fairhurst, Robin A, Fozard, John R, Gedeck, Peter, Kirkham, Paul, Meja, Koremu, Nanson, Lana, Neef, James, Oakman, Helen, Spooner, Gillian, Taylor, Roger J, Turner, Robert J, West, Ryan and Woodward, Hannah (2010) Synthesis and evaluation of two series of 4′-aza-carbocyclic nucleosides as adenosine A2A receptor agonists. Bioorganic and Medicinal Chemistry Letters, 20 (3). pp. 1219-1224. ISSN 0960-894X

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Abstract

The synthesis of two series of 4′-aza-carbocyclic nucleosides are described in which the 4′-substituent is either a reversed amide, relative to the carboxamide of NECA, or an N-bonded heterocycle. Using established purine substitution patterns, potent and selective examples of agonists of the human adenosine A2A receptor have been identified from both series. The propionamides 14–18 and the 4-hydroxymethylpyrazole 32 were determined to be the most potent and selective examples from the 4′-reversed amide and 4′-N-bonded heterocyclic series, respectively.

Item Type: Article
Schools and Departments: School of Life Sciences > Chemistry
Subjects: Q Science > QD Chemistry
Depositing User: Tom Gittoes
Date Deposited: 12 Jan 2015 15:40
Last Modified: 12 Jan 2015 15:40
URI: http://sro.sussex.ac.uk/id/eprint/52051
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