Insight into 2-phenylpyrazolo[1,5-a]pyrimidin-3-yl acetamides as Peripheral Benzodiazepine Receptor Ligands: synthesis, biological evaluation and 3D-QSAR investigation.

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.