3-Arylpiperazinylethyl-1H-pyrrolo[2,3-d]pyrimidine-2,4(3H,7H)-dione derivatives as novel, high-affinity and selective α1- adrenoceptor ligands

Abstract The discovery of a new series of selective and high-affinity α 1 -adrenoceptor (α 1 -AR) ligands, characterized by a 1 H -pyrrolo[2,3- d ]-pyrimidine-2,4(3 H ,7 H )-dione system, is described in this paper. Some synthesized compounds, including 20 , 22 , and 30 , displayed affinity in the nanomolar range for α 1 -ARs and substantial selectivity with respect to 5-HT 1A and dopaminergic D 1 and D 2 receptors. Functional assays, performed on selected derivatives, showed antagonistic properties.