title: Norbornyllactone-substituted xanthines as adenosine A(1) receptor antagonists.
abstract: 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.
authors.affiliation: Department of Medicinal Chemistry, Biogen Idec, Inc., 14 Cambridge Center, Cambridge, MA 02142, USA. william.kiesman@biogenidec.com
authors.forename: William F
authors.initials: WF
authors.lastname: Kiesman
authors.forename: Jin
authors.initials: J
authors.lastname: Zhao
authors.forename: Patrick R
authors.initials: PR
authors.lastname: Conlon
authors.forename: Russell C
authors.initials: RC
authors.lastname: Petter
authors.forename: Xiaowei
authors.initials: X
authors.lastname: Jin
authors.forename: Glenn
authors.initials: G
authors.lastname: Smits
authors.forename: Frank
authors.initials: F
authors.lastname: Lutterodt
authors.forename: Gail W
authors.initials: GW
authors.lastname: Sullivan
authors.forename: Joel
authors.initials: J
authors.lastname: Linden
mesh_terms: D058916:Adenosine A1 Receptor Antagonists; D058917:Adenosine A2 Receptor Antagonists; D058918:Adenosine A3 Receptor Antagonists; D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001643:Bridged Bicyclo Compounds / Q000737:chemistry*; D002460:Cell Line; D006801:Humans; D007783:Lactones / Q000737:chemistry*; D008024:Ligands; D015394:Molecular Structure; D009636:Norbornanes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014970:Xanthines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D058916:Adenosine A1 Receptor Antagonists; D058917:Adenosine A2 Receptor Antagonists; D058918:Adenosine A3 Receptor Antagonists; D001643:Bridged Bicyclo Compounds; D007783:Lactones; D008024:Ligands; D009636:Norbornanes; D014970:Xanthines; C512315:norbornyllactone