Discovery of the first A1 adenosine receptor ligand based on the chromone scaffold

摘要

The first potent and selective hA _(1) AR ligand based on the chromone scaffold is reported in this work. Receptor-driven molecular modeling studies provide valuable information about the molecular interactions responsible for the high affinity of N -(2-nitrophenyl)-4-oxo-4 H -chromene-2-carboxamide to the hA _(1) AR ( K _(i) = 0.219 μM) and reinforce the crucial role of AR affinity of the amide linker located at C-2 of the pyrone ring.