Title of article :
3-Arylpiperazinylethyl-1H-pyrrolo[2,3-d]pyrimidine-2,4(3H,7H)-dione derivatives as novel, high-affinity and selective α1-adrenoceptor ligands
Author/Authors :
Valeria Pittalà، نويسنده , , Giuseppe Romeo، نويسنده , , Loredana Salerno، نويسنده , , Maria Angela Siracusa، نويسنده , , Maria Modica، نويسنده , , Luisa Materia، نويسنده , , Ilario Mereghetti، نويسنده , , Alfredo Cagnotto، نويسنده , , Tiziana Mennini، نويسنده , , Gabriella Marucci، نويسنده , , Piero Angeli، نويسنده , , Filippo Russo، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2006
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.
Keywords :
?1-Adrenoceptor subtypes , 3-d]pyrimidine-2 , Arylpiperazine , 7H)-dione , 4(3H , ?1-Adrenoceptor antagonists
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
