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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetamides / chemical synthesis
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Acetamides / chemistry*
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Acetamides / pharmacology*
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Animals
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Cell Line, Tumor
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Cells, Cultured
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GABA-A Receptor Antagonists
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Glioma / metabolism
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Kidney / cytology
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Kidney / metabolism
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Ligands
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Magnetic Resonance Spectroscopy
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Male
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Models, Molecular
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Molecular Probes
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Molecular Structure
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Pyrimidines / chemical synthesis
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Pyrimidines / chemistry
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Pyrimidines / pharmacology
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Quantitative Structure-Activity Relationship
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Rats
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Rats, Wistar
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Receptors, GABA-A / chemistry*
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Receptors, GABA-A / metabolism*
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Steroids / biosynthesis
Substances
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Acetamides
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GABA-A Receptor Antagonists
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Ligands
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Molecular Probes
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Pyrimidines
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Receptors, GABA-A
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Steroids