Abstract
A new series of potential adenosine receptor antagonists with a 1,2,4-triazolo-3,4-f-purine
structure bearing at the 1 and 3 position n-propyl groups have been
synthesized, and their affinities at the four human adenosine receptor
subtypes (A(1), A(2A), A(2B) and A(3)) have been evaluated. In this
case the presence of n-propyl groups seems to induce potency at the
A(2A) and A(3) adenosine receptor subtypes as opposed to our previously
reported series bearing methyl substituents at the 1 and 3 positions.
In particular the non-acylated derivative 17 showed affinity at these
two receptor subtypes in the micromolar range. Indeed, preliminary
molecular modeling investigations according to the experimental binding
data indicate a modest steric and electrostatic antagonist-receptor
complementarity.
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