Literature DB >> 17234414

3H-[1,2,4]-Triazolo[5,1-i]purin-5-amine derivatives as adenosine A2A antagonists.

Lisa S Silverman1, John P Caldwell, William J Greenlee, Eugenia Kiselgof, Julius J Matasi, Deen B Tulshian, Leyla Arik, Carolyn Foster, Rosalia Bertorelli, Angela Monopoli, Ennio Ongini.   

Abstract

A novel series of 3-substituted-8-aryl-[1,2,4]-triazolo[5,1-i]purin-5-amine analogs related to Sch 58261 was synthesized in order to identify potent adenosine A(2A) receptor antagonists with improved selectivity over the A(1) receptor, physiochemical properties, and pharmacokinetic profiles as compared to those of Sch 58261. As a result of structural modifications, numerous analogs with excellent in vitro binding affinities and selectivities were identified. Moreover, compound 27 displayed both superior in vitro and highly promising in vivo profiles.

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Year:  2007        PMID： 17234414     DOI： 10.1016/j.bmcl.2006.12.104

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


  3 in total

1.  Synthesis of purine modified 2'-C-methyl nucleosides as potential anti-HCV agents.

Authors:  Hong-wang Zhang; Longhu Zhou; Steven J Coats; Tamara R McBrayer; Phillip M Tharnish; Lavanya Bondada; Mervi Detorio; Sarah A Amichai; Melissa D Johns; Tony Whitaker; Raymond F Schinazi
Journal:  Bioorg Med Chem Lett       Date:  2011-09-20       Impact factor: 2.823

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

3.  Piperazine- and Piperidine-Containing Thiazolo[5,4-d]pyrimidine Derivatives as New Potent and Selective Adenosine A2A Receptor Inverse Agonists.

Authors:  Flavia Varano; Daniela Catarzi; Erica Vigiani; Fabrizio Vincenzi; Silvia Pasquini; Katia Varani; Vittoria Colotta
Journal:  Pharmaceuticals (Basel)       Date:  2020-07-24
  3 in total

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