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Synthesis and Evaluation of Two Series of 4'-Aza-Carbocyclic Nucleosides as Adenosine A2A Receptor Agonists

Beattie, David and Brearley, Andrew and Brown, Zarin and Charlton, Steven and Cox, Brian and Fairhurst, Robin and Fozard, John R. and Gedeck, Peter and Kirkham, Paul and Meja, Koremu and Nanson, Lana and Neef, James and Oakman, Helen and Taylor, Roger and Turner, Robert and 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

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.

Item Type: Article
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Additional Information: These series of 4'-azacarbocyclic nucleosides have already been disclosed in the following patent filings: WO 2006/045552, WO 2006/074925, WO 2007/121920, WO 2007/121917, WO 2007/121921, WO 2007/121923, WO 2007/121919, WO 2007/121924, WO 2007/147659, WO 2008/031865, WO 2008/006563, WO 2009/050198, WO 2009/050199
Keywords: Adenosine A2A receptor agonists carbocyclic nucleosides
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Date Deposited: 13 Oct 2015 13:17
Last Modified: 13 Oct 2015 13:17
URI: https://oak.novartis.com/id/eprint/1127

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