Flavylium salts as in vitro precursors of potent ligands to brain GABA-A receptors

Bioorganic & Medicinal Chemistry Letters
Marie Kueny-StotzMaurice Goeldner

Abstract

The synthesis of a series of derivatized flavylium cations was undertaken and the affinity to the benzodiazepine binding site of the GABA-A receptor evaluated. The observed high affinity for some derivatives (sub-muM range) was explained by an in vitro transformation of the flavylium cations into the corresponding trans-retrochalcones, components which are proposed to be the active species in this series.

References

Aug 1, 1992·Proceedings of the National Academy of Sciences of the United States of America·J M FritschyH Möhler
Jan 1, 1994·Annual Review of Neuroscience·R L Macdonald, R W Olsen
Mar 29, 2000·Bioscience, Biotechnology, and Biochemistry·T DeguchiS Ueda
Apr 26, 2000·Journal of Medicinal Chemistry·M Chebib, G A Johnston
Mar 23, 2001·Journal of Agricultural and Food Chemistry·S MeiersD Marko
Jul 20, 2002·Progress in Neurobiology·Esa R KorpiHartmut Lüddens
Aug 13, 2002·Current Topics in Medicinal Chemistry·Mariel Marder, Alejandro C Paladini
Jun 25, 2005·Current Pharmaceutical Design·Graham A R Johnston

❮ Previous
Next ❯

Citations

Sep 26, 2015·SpringerPlus·Homar S BarcenaAbraham Tuachi
Jul 30, 2016·Journal of the American Chemical Society·Zhenyu YangF Dean Toste
Jun 28, 2017·Journal of Medicinal Chemistry·José M EstrelaRyan W Dellinger
Mar 15, 2020·Molecular Diversity·Kavita BhagatPreet Mohinder S Bedi
Nov 30, 2021·Chemical Reviews·Luis CruzFernando Pina

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.