Abstract
The discovery of new drugs for the treatment of neurodegenerative
disorders, such as Parkinson's disease, has become an attractive
field of research. Due to the regulation of D(2) receptor activity
by A(2A) adenosine receptor, potent and selective ligands of A(2A)
subtype could be useful tools to study neurodegenerative disorders.
A series of 2,8-disubstituted-9-ethyladenine derivatives was synthesized
and tested in binding affinity assay at human adenosine receptors.
New compounds showed good affinity and selectivity at A(2A) receptor
versus the other subtypes. The introduction of a bromine atom in
8-position increased the affinity of these compounds, leading to
ligands with K(i) in the nanomolar range.
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