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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

GABA-A-Receptor Ligands of Flavonoid Structure

Author(s): Mariel Marder and Alejandro C. Paladini

Volume 2, Issue 8, 2002

Page: [853 - 867] Pages: 15

DOI: 10.2174/1568026023393462

Price: $65


This review describes the new research developments that have established the CNS-activity of some natural flavonoids. The properties of flavone, chrysin, apigenin and cirsiliol are described and a survey of the occurrence of ligands for the benzodiazepine binding site in the flavonoid field is attempted. Natural compounds, structurally related to flavonoids and with similar CNS-activities, are also included. A medicinal chemistry approach to improve the biochemical and pharmacological properties of the flavone nucleus is described alongside with the enumeration of the principal achievements obtained to date. Quantitative structure-activity relationships studies leading to the formulation of pharmacophore models presumably describing the characteristics of the flavone-binding site in the GABA-A -receptor are summarized.

Keywords: gaba ligand, flavone-binding site

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