title: Synthesis and pharmacological evaluation of novel substituted 9-deazaxanthines as A2B receptor antagonists.
abstract: A new series of 9-deazaxanthine derivatives with various substituents at the heterocyclic system were synthesized and evaluated for their binding affinities for the four human recombinant adenosine receptors, A(1)-A(3) subtypes. A number of the 9-deazaxanthines derivatives 3a-m showed moderate-to-high affinity for hA(2B) receptors, with compound 3f showing a 32-fold selectivity for A(2B) over A(1) and a 2750-fold selectivity for A(2B) over A(2A).
authors.affiliation: Departamento de Química Fundamental, Facultade de Química, Universidade de A Coruña, Campus da Zapateira, E-15071, A Coruña, Spain.
authors.forename: María Isabel
authors.initials: MI
authors.lastname: Nieto
authors.forename: María Carmen
authors.initials: MC
authors.lastname: Balo
authors.forename: José
authors.initials: J
authors.lastname: Brea
authors.forename: Olga
authors.initials: O
authors.lastname: Caamaño
authors.forename: Franco
authors.initials: F
authors.lastname: Fernández
authors.forename: Xerardo
authors.initials: X
authors.lastname: García-Mera
authors.forename: Carmen
authors.initials: C
authors.lastname: López
authors.forename: María Isabel
authors.initials: MI
authors.lastname: Loza
authors.forename: José Enrique
authors.initials: JE
authors.lastname: Rodríguez-Borges
authors.forename: Bernat
authors.initials: B
authors.lastname: Vidal
mesh_terms: D058917:Adenosine A2 Receptor Antagonists; D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D006367:HeLa Cells; D006801:Humans; D008024:Ligands; D014970:Xanthines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D058917:Adenosine A2 Receptor Antagonists; D008024:Ligands; D014970:Xanthines