Discovery of FK453, a novel non-xanthine adenosine A1 receptor antagonist

Article abstract of DOI:10.1016/0960-894X(96)00368-X

Novel 2-phenylpyrazolo[1,5-a]pyridine-3-acryloylamides were synthesized and evaluated for diuretic activities. FK453 (1d), the most potent compound in this series, was found to be a potent and selective adenosine A₁ receptor antagonist, whereas 1e, the (S)-enantiomer of FK453, was a weak and non-selective adenosine antagonist.