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

…, L Materia, I Mereghetti, A Cagnotto, T Mennini…

文献索引：Pittala, Valeria; Romeo, Giuseppe; Salerno, Loredana; Siracusa, Maria Angela; Modica, Maria; Materia, Luisa; Mereghetti, Ilario; Cagnotto, Alfredo; Mennini, Tiziana; Marucci, Gabriella; Angeli, Piero; Russo, Filippo Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 1 p. 150 - 153

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被引用次数: 12

摘要

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 ...