Literature DB >> 19059776

Synthesis of 2-amino-5-benzoyl-4-(2-furyl)thiazoles as adenosine A(2A) receptor antagonists.

Andrew G Cole1, Tara M Stauffer, Laura L Rokosz, Axel Metzger, Lawrence W Dillard, Wenguang Zeng, Ian Henderson.   

Abstract

The discovery and synthesis of a series of 2-amino-5-benzoyl-4-(2-furyl)thiazoles as adenosine A(2A) receptor antagonists from a small-molecule combinatorial library using a high-throughput radioligand-binding assay is described. Antagonists were further characterized in the A(2A) binding assay and an A(1) selectivity assay. Selected examples exhibited excellent affinity for A(2A) and good selectivity versus the A(1) receptor.

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Year:  2008        PMID: 19059776     DOI: 10.1016/j.bmcl.2008.11.066

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009.

Authors:  Roland E Dolle; Bertrand Le Bourdonnec; Karin Worm; Guillermo A Morales; Craig J Thomas; Wei Zhang
Journal:  J Comb Chem       Date:  2010-10-05

Review 2.  Adenosine A(2A) Receptor Antagonists and Parkinson's Disease.

Authors:  Brian C Shook; Paul F Jackson
Journal:  ACS Chem Neurosci       Date:  2011-06-21       Impact factor: 4.418

  2 in total

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