Pittalà, Valeria, Romeo, Giuseppe, Salerno, Loredana, Siracusa, Maria Angela, Modica, Maria, Materia, Luisa, Mereghetti, Ilario, Cagnotto, Alfredo, Mennini, Tiziana, Marucci, Gabriella, Angeli, Piero, and Russo, Filippo
Abstract: The discovery of a new series of selective and high-affinity α1-adrenoceptor (α1-AR) ligands, characterized by a 1H-pyrrolo[2,3-d]-pyrimidine-2,4(3H,7H)-dione system, is described in this paper. Some synthesized compounds, including 20, 22, and 30, displayed affinity in the nanomolar range for α1-ARs and substantial selectivity with respect to 5-HT1A and dopaminergic D1 and D2 receptors. Functional assays, performed on selected derivatives, showed antagonistic properties. [Copyright &y& Elsevier]