Kiesman William F, Zhao Jin, Conlon Patrick R, Petter Russell C, Jin Xiaowei, Smits Glenn, Lutterodt Frank, Sullivan Gail W, Linden Joel
Department of Medicinal Chemistry, Biogen Idec, Inc., 14 Cambridge Center, Cambridge, MA 02142, USA.
Bioorg Med Chem. 2006 Jun 1;14(11):3654-61. doi: 10.1016/j.bmc.2006.01.021. Epub 2006 Feb 2.
During the search for second-generation adenosine A(1) receptor antagonist alternatives to the clinical candidate 8-(3-oxa-tricyclo[3.2.1.0(2,4)]oct-6-yl)-1,3-dipropyl-3,7-dihydro-purine-2,6-dione (BG9719), we developed a series of novel xanthines substituted with norbornyl-lactones that possessed high binding affinities for adenosine A(1) receptors and in vivo activity.
在寻找临床候选药物8-(3-氧杂-三环[3.2.1.0(2,4)]辛-6-基)-1,3-二丙基-3,7-二氢嘌呤-2,6-二酮（BG9719）的第二代腺苷A(1)受体拮抗剂替代品的过程中，我们开发了一系列用降冰片基内酯取代的新型黄嘌呤，这些黄嘌呤对腺苷A(1)受体具有高结合亲和力和体内活性。
