Synthesis and Evaluation of Two Series of 4'-Aza-Carbocyclic Nucleosides as Adenosine A2A Receptor Agonists
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Beattie, David, Brearley, Andrew, Brown, Zarin, Charlton, Steven, Cox, Brian, Fairhurst, Robin, Fozard, John R., Gedeck, Peter, Kirkham, Paul, Meja, Koremu, Nanson, Lana, Neef, James, Oakman, Helen, Taylor, Roger, Turner, Robert, 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 |