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XH-14 analogues as adenosine antagonists
P J Scammells1, S P Baker, A R Beauglehole
1School of Biological and Chemical Sciences, Deakin University, Geelong, VIC, Australia. scam@deakin.edu.au
Bioorganic & Medicinal Chemistry
|November 5, 1998
Abstract:
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.