Abstract
A new series of potential adenosine receptor antagonists with a 1,2,4-triazolo-3,4-f-purine
structure have been synthesized, and their affinities at the four
adenosine receptor subtypes (A1, A2A, A2B and A3) have been evaluated.
The design was based on the demonstrated approach to novel A3 adenosine
receptor antagonists of adding a third ring to the xanthine structure.
Unfortunately, all the synthesized compounds were completely inactive
at all four adenosine receptor subtypes independently of their substitutions.
Preliminary molecular modeling investigation has demonstrated that
only a low degree of steric and electrostatic complementarity has
been observed for all the new synthesized triazolo-purines with respect
to other structurally related A3 receptor antagonists. This analysis
yielded valuable information about structure-activity relationships
and further design of potential adenosine receptor antagonists.
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