Synthesis and pharmacological evaluation of novel substituted 9-deazaxanthines as A2B receptor antagonists.
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).
Nieto
María Isabel
MI
Departamento de Química Fundamental, Facultade de Química, Universidade de A Coruña, Campus da Zapateira, E-15071, A Coruña, Spain.
Balo
María Carmen
MC
Brea
José
J
Caamaño
Olga
O
Fernández
Franco
F
García-Mera
Xerardo
X
López
Carmen
C
Loza
María Isabel
MI
Rodríguez-Borges
José Enrique
JE
Vidal
Bernat
B
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*
D058917:Adenosine A2 Receptor Antagonists; D008024:Ligands; D014970:Xanthines