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Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists
journal contributionposted 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.
JournalBioorganic and Medicinal Chemistry Letters
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- Chemistry Publications
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