Title of article :
Insight into 2-phenylpyrazolo[1,5-a]pyrimidin-3-yl acetamides as peripheral benzodiazepine receptor ligands: Synthesis, biological evaluation and 3D-QSAR investigation Original Research Article
Author/Authors :
Silvia Selleri، نويسنده , , Paola Gratteri، نويسنده , , Camilla Costagli، نويسنده , , Claudia Bonaccini، نويسنده , , Annarella Costanzo، نويسنده , , Fabrizio Melani، نويسنده , , Gabriella Guerrini، نويسنده , , Giovanna Ciciani، نويسنده , , Barbara Costa، نويسنده , , Francesca Spinetti، نويسنده , , Claudia Martini، نويسنده , , Fabrizio Bruni، نويسنده ,
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.
Keywords :
Aminopeptidase P , slow-binding inhibition , Bestatin , Mixed-type inhibition
