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Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists. 2010
David Beattie, and
Andrew Brearley, and
Zarin Brown, and
Steven J Charlton, and
Brian Cox, and
Robin A Fairhurst, and
John R Fozard, and
Peter Gedeck, and
Paul Kirkham, and
Koremu Meja, and
Lana Nanson, and
James Neef, and
Helen Oakman, and
Gillian Spooner, and
Roger J Taylor, and
Robert J Turner, and
Ryan West, and
Hannah Woodward
Novartis Institutes for BioMedical Research, Respiratory Diseases Area, Horsham, United Kingdom.
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 A(2A) 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.
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