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

journal contribution
posted on 2023-06-08, 19:29 authored by David Beattie, Andrew Brearley, Zarin Brown, Steven J Charlton, Brian Cox, Robin A Fairhurst, John R Fozard, Peter Gedeck, Paul Kirkham, Koremu Meja, Lana Nanson, James Neef, Helen Oakman, Gillian Spooner, Roger J Taylor, Robert J Turner, Ryan West, Hannah Woodward
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.

History

Publication status

  • Published

Journal

Bioorganic and Medicinal Chemistry Letters

ISSN

0960-894X

Publisher

Elsevier

Issue

3

Volume

20

Page range

1219-1224

Department affiliated with

  • Chemistry Publications

Full text available

  • No

Peer reviewed?

  • Yes

Legacy Posted Date

2015-01-12

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