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Bioorg Med Chem Lett. 2010 Feb 1;20(3):1219-24. doi: 10.1016/j.bmcl.2009.11.131. Epub 2009 Dec 1.

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

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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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