Detection of Benzodiazepine Receptor Ligands in Small Libraries of Flavone Derivatives Synthesized by Solution Phase Combinatorial Chemistry

Solution phase combinatorial synthesis of flavone derivatives and evaluation of their affinity for the central benzodiazepine receptors is described. The libraries preparation is simple and provides a convenient method for rapid compound generation and screening. Thirty one new compounds were obtain...

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Bibliographic Details
Published in:Biochemical and biophysical research communications 1998-08, Vol.249 (2), p.481-485
Main Authors: Marder, Mariel, Viola, Haydee, Bacigaluppo, José A., Colombo, Marı́a I., Wasowski, Cristina, Wolfman, Claudia, Medina, Jorge H., Rúveda, Edmundo A., Paladini, Alejandro C.
Format: Article
Language:English
Subjects:
Animals
Binding, Competitive
Cell Membrane - metabolism
Cerebellum - metabolism
Cerebral Cortex - metabolism
Chromatography, High Pressure Liquid
Flavonoids - chemical synthesis
Flavonoids - chemistry
Flavonoids - metabolism
Flunitrazepam - metabolism
gamma-Aminobutyric Acid - metabolism
Mice
Molecular Structure
Rats
Receptors, GABA-A - metabolism
Solutions
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Summary:Solution phase combinatorial synthesis of flavone derivatives and evaluation of their affinity for the central benzodiazepine receptors is described. The libraries preparation is simple and provides a convenient method for rapid compound generation and screening. Thirty one new compounds were obtained of which the most promising, as high affinity benzodiazepine receptor ligands, were 6-bromo-3′-fluoroflavone; 6,3′-dichloroflavone; 6-bromo-3′-chloroflavone and 6-chloro-3′-bromoflavone.
ISSN:0006-291X
1090-2104
DOI:10.1006/bbrc.1998.9146