Zhu Ran, Frazier Cynthia R, Linden Joel, Macdonald Timothy L
Department of Chemistry, University of Virginia, Charlottesville, VA 22904-4319, USA.
Bioorg Med Chem Lett. 2006 May 1;16(9):2416-8. doi: 10.1016/j.bmcl.2006.01.110. Epub 2006 Feb 17.
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.
合成了一系列N6-乙基-2-炔基NECA（5'-N-乙基甲酰胺基腺苷）类似物，并评估了它们与四种人类腺苷受体的结合亲和力。其中一种化合物ZR1121对hA3受体显示出高亲和力，并且其对hA1受体的选择性比目前使用的选择性A3激动剂IB-MECA或Cl-IB-MECA高1-2个对数级。
