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

• DOI: 10.1006/bbrc.1998.9146
• Publication Date: 2002-09-16T14:49:55Z
• Authors: Mariel Marder; Haydee Viola; José A. Bacigaluppo; Marı́a I. Colombo; Cristina Wasowski; Claudia Wolfman; Jorge H. Medina; Edmundo A. Rúveda; Alejandro C. Pala...
• Keywords: Cerebral Cortex; Flavonoids; 0301 basic medicine; Molecular Structure; Cell Membrane; Flunitrazepam; Receptors, GABA-A; Binding, Competitive; Rats; 3. Good health; Solutions; Mice; 03 medical and health sciences; Cerebellum; Animals; Chromatography, High Pressure Liquid; gamma-Aminobutyric Acid

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.