Insight into 2-phenylpyrazolo[1,5-a]pyrimidin-3-yl acetamides as peripheral benzodiazepine receptor ligands: Synthesis, biological evaluation and 3D-QSAR investigation

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• 作者：Silvia Selleri ; Paola Gratteri ; Camilla Costagli ; Claudia Bonaccini ; Annarella Costanzo ; Fabrizio Melani ; Gabriella Guerrini ; Giovanna Ciciani ; Barbara Costa ; Francesca Spinetti et al.
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2005
• 出版时间：2005
• 年：2005
• 卷：13
• 期：16
• 页码：4821-4834
• 全文大小：1233 K

文摘

The present paper reports the synthesis and binding studies of new 2-phenylpyrazolo[1,5-a]pyrimidin-3-yl acetamides as selective Peripheral Benzodiazepine Receptor (PBR) ligands. The variability of substituents at the 3-position was investigated and a 3D-QSAR model was proposed to evaluate the effect of different substitutions on the acetamide moiety. In addition, a subset of the novel compounds showing high affinity for PBR was tested for their ability to modulate the steroid biosynthesis in C6 glioma cells.