2. Academic Validation
  3. N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists

N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists

  • Bioorg Med Chem Lett. 2006 May 1;16(9):2416-8. doi: 10.1016/j.bmcl.2006.01.110.
Ran Zhu 1,  Cynthia R Frazier,  Joel Linden,  Timothy L Macdonald
Affiliations

Affiliation

  • 1 Department of Chemistry, University of Virginia, Charlottesville, VA 22904-4319, USA.
PMID: 16487705 DOI: 10.1016/j.bmcl.2006.01.110
Abstract

A series of N6-ethyl-2-alkynyl NECA (5'-N-ethylcarboxamidoadenosine) analogs were synthesized and their binding affinity with the four human adenosine receptors was evaluated. One of the compounds ZR1121 shows high affinity with hA3 receptor and its selectivity over hA1 receptor is 1-2 log orders greater than IB-MECA or Cl-IB-MECA, the currently employed selective A3 agonists.

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