Literature DB >> 15876531

A new orally bioavailable dual adenosine A2B/A3 receptor antagonist with therapeutic potential.

Neil J Press1, Roger J Taylor, Joseph D Fullerton, Pamela Tranter, Clive McCarthy, Thomas H Keller, Lyndon Brown, Robert Cheung, Julie Christie, Sandra Haberthuer, Julia D I Hatto, Mark Keenan, Mark K Mercer, Nicola E Press, Helene Sahri, Andrew R Tuffnell, Morris Tweed, John R Fozard.   

Abstract

The synthesis and SAR of 5-heterocycle-substituted aminothiazole adenosine receptor antagonists is described. Several compounds show high affinity and selectivity for the A2B and A3 receptors. One compound (5f) shows good ADME properties in the rat and as such may be an important new compound in testing the current hypotheses proposing a therapeutic role for a dual A2B/A3 antagonist in allergic diseases.

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Year:  2005        PMID: 15876531     DOI: 10.1016/j.bmcl.2005.04.021

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


  6 in total

Review 1.  Adenosine receptors as therapeutic targets.

Authors:  Kenneth A Jacobson; Zhan-Guo Gao
Journal:  Nat Rev Drug Discov       Date:  2006-03       Impact factor: 84.694

Review 2.  Adenosine receptors and asthma.

Authors:  Constance N Wilson; Ahmed Nadeem; Domenico Spina; Rachel Brown; Clive P Page; S Jamal Mustafa
Journal:  Handb Exp Pharmacol       Date:  2009

Review 3.  Introduction to adenosine receptors as therapeutic targets.

Authors:  Kenneth A Jacobson
Journal:  Handb Exp Pharmacol       Date:  2009

4.  Structure-activity relationships of 2-aminothiazoles effective against Mycobacterium tuberculosis.

Authors:  Anja Meissner; Helena I Boshoff; Mahalakshmi Vasan; Benjamin P Duckworth; Clifton E Barry; Courtney C Aldrich
Journal:  Bioorg Med Chem       Date:  2013-09-03       Impact factor: 3.641

5.  Discovery of 2-aminothiazoles as potent antiprion compounds.

Authors:  Sina Ghaemmaghami; Barnaby C H May; Adam R Renslo; Stanley B Prusiner
Journal:  J Virol       Date:  2009-12-23       Impact factor: 5.103

Review 6.  Successes and challenges in phenotype-based lead discovery for prion diseases.

Authors:  Sina Ghaemmaghami; Miranda Russo; Adam R Renslo
Journal:  J Med Chem       Date:  2014-04-24       Impact factor: 7.446

  6 in total

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