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

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• 作者：Valeria Pittalà ; Giuseppe Romeo ; Loredana Salerno ; Maria Angela Siracusa ; Maria Modica ; Luisa Materia ; Ilario Mereghetti ; Alfredo Cagnotto ; Tiziana Mennini ; Gabriella Marucci et al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 January 2006
• 卷：16
• 期：1
• 页码：150-153
• 文件大小：116 K

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-HT_1A and dopaminergic D₁ and D₂ receptors. Functional assays, performed on selected derivatives, showed antagonistic properties.