GABA-A-Receptor Ligands of Flavonoid Structure
- 1 August 2002
- journal article
- review article
- Published by Bentham Science Publishers Ltd. in Current Topics in Medicinal Chemistry
- Vol. 2 (8) , 853-867
- https://doi.org/10.2174/1568026023393462
Abstract
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
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