Synthesis and evaluation of adenosine antagonist activity of a series of [1,2,4]triazolo[1,5-c]quinazolines.
A series of [1,2,4]triazolo[1,5-c]quinazolines were prepared in satisfactory yields by reaction of some derivatives of 2-aminobenzohydrazide with several hydrochlorides of aromatic amidines, and their binding affinities for the recombinant human adenosine A2A and A2B receptors were determined. None of the new compounds showed noteworthy affinity for these receptors, though a very high affinity for the A2A receptor and, consequently, a high level of A2A/A2B selectivity was revealed for one of the synthesized compounds.
Balo
Carmen
C
Departamento de Química Orgánica, Facultade de Farmacia, Universidade de Santiago de Compostela, Santiago de Compostela, Spain.
López
Carmen
C
Brea
José Manuel
JM
Fernández
Franco
F
Caamaño
Olga
O
D058917:Adenosine A2 Receptor Antagonists; D006801:Humans; D015394:Molecular Structure; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D043705:Receptor, Adenosine A2A / Q000737:chemistry / Q000378:metabolism; D043704:Receptor, Adenosine A2B / Q000737:chemistry / Q000378:metabolism; D011994:Recombinant Proteins; D013329:Structure-Activity Relationship
D058917:Adenosine A2 Receptor Antagonists; D011799:Quinazolines; D043705:Receptor, Adenosine A2A; D043704:Receptor, Adenosine A2B; D011994:Recombinant Proteins