Synthesis and Evaluation of Adenosine Antagonist Activity of a Series of [1,2,4]Triazolo[1,5-c]quinazolines

抄録

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 A_2A and A_2B receptors were determined. None of the new compounds showed noteworthy affinity for these receptors, though a very high affinity for the A_2A receptor and, consequently, a high level of A_2A/A_2B selectivity was revealed for one of the synthesized compounds.