XH-14 analogues as adenosine antagonists Original Research Article

Analogues of the potent adenosine antagonist 5-(3′-hydroxypropyl)-7-methoxy-2-(3′-methoxy-4′-hydroxyphenyl)benzo[b]furan-3-carbaldehyde (XH-14, 1) with alternate substituents in the 2-, 5- and 7-positions have been synthesised. The affinity of these compounds for the A1 adenosine receptor has been evaluated using a [3H]CPX competitive binding assay. This structure-activity study highlighted the importance of the 3-formyl and 5-(3-hydroxypropyl) moieties for high receptor affinity.