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  • Title: Insight into 2-phenylpyrazolo[1,5-a]pyrimidin-3-yl acetamides as peripheral benzodiazepine receptor ligands: synthesis, biological evaluation and 3D-QSAR investigation.
    Author: Selleri S, Gratteri P, Costagli C, Bonaccini C, Costanzo A, Melani F, Guerrini G, Ciciani G, Costa B, Spinetti F, Martini C, Bruni F.
    Journal: Bioorg Med Chem; 2005 Aug 15; 13(16):4821-34. PubMed ID: 15975799.
    Abstract:
    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.
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