Literature DB >> 20652178

An efficient route to xanthine based A(2A) adenosine receptor antagonists and functional derivatives.

Paul Labeaume1, Ma Dong, Michail Sitkovsky, Elizabeth V Jones, Rhiannon Thomas, Sara Sadler, Amy E Kallmerten, Graham B Jones.   

Abstract

A one-pot route to 8-substituted xanthines has been developed from 5,6-diaminouracils and carboxaldehydes. Yields are good and the process applicable to a range of substrates including a family of A(2A) adenosine receptor antagonists. A new route to the KW-6002 family of antagonists is presented including a pro-drug variant, and application to related image contrast agents developed.

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Year:  2010        PMID: 20652178     DOI: 10.1039/c003382k

Source DB:  PubMed          Journal:  Org Biomol Chem        ISSN: 1477-0520            Impact factor:   3.876


  1 in total

1.  Design and evaluation of xanthine based adenosine receptor antagonists: potential hypoxia targeted immunotherapies.

Authors:  Rhiannon Thomas; Joslynn Lee; Vincent Chevalier; Sara Sadler; Kaisa Selesniemi; Stephen Hatfield; Michail Sitkovsky; Mary Jo Ondrechen; Graham B Jones
Journal:  Bioorg Med Chem       Date:  2013-09-28       Impact factor: 3.641

  1 in total

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