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Issue 4, 2013
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Methanocarba ring as a ribose modification in ligands of G protein-coupled purine and pyrimidine receptors: synthetic approaches

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Abstract

Adenosine receptors (ARs) and P2Y receptors for purine and pyrimidine nucleotides have widespread distribution and regulate countless physiological processes. Various synthetic ligands are in clinical trials for treatment of inflammatory diseases, pain, cancer, thrombosis, ischemia, and other conditions. The methanocarba (bicyclo[3.1.0]hexane) ring system as a rigid substitution for ribose, which maintains either a North (N) or South (S) conformation, tends to preserve or enhance the potency and/or selectivity for certain receptor subtypes. This review summarizes recent developments in the synthetic approaches to these biologically important nucleoside and nucleotide analogues.

Graphical abstract: Methanocarba ring as a ribose modification in ligands of G protein-coupled purine and pyrimidine receptors: synthetic approaches

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Publication details

The article was received on 20 Nov 2012, accepted on 13 Dec 2012 and first published on 17 Dec 2012


Article type: Review Article
DOI: 10.1039/C2MD20348K
Med. Chem. Commun., 2013,4, 619-630

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    Methanocarba ring as a ribose modification in ligands of G protein-coupled purine and pyrimidine receptors: synthetic approaches

    D. K. Tosh and K. A. Jacobson, Med. Chem. Commun., 2013, 4, 619
    DOI: 10.1039/C2MD20348K

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