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: gaba ligand, flavone-binding site
Current Topics in Medicinal Chemistry
Title: GABA-A-Receptor Ligands of Flavonoid Structure
Volume: 2 Issue: 8
Author(s): Mariel Marder and Alejandro C. Paladini
Affiliation:
Keywords: gaba ligand, flavone-binding site
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.
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Cite this article as:
Marder Mariel and Paladini C. Alejandro, GABA-A-Receptor Ligands of Flavonoid Structure, Current Topics in Medicinal Chemistry 2002; 2 (8) . https://dx.doi.org/10.2174/1568026023393462
DOI https://dx.doi.org/10.2174/1568026023393462 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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