Flavylium salts as in vitro precursors of potent ligands to brain GABA-A receptors
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Flavylium salts as in vitro precursors of potent ligands to brain GABA-A receptors. / Kueny-Stotz, Marie; Chassaing, Stefan; Brouillard, Raymond; Nielsen, Mogens Peter Cherly; Goeldner, Maurice.
In: Bioorganic & Medicinal Chemistry Letters, Vol. 18, No. 17, 2008, p. 4864-4867.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Flavylium salts as in vitro precursors of potent ligands to brain GABA-A receptors
AU - Kueny-Stotz, Marie
AU - Chassaing, Stefan
AU - Brouillard, Raymond
AU - Nielsen, Mogens Peter Cherly
AU - Goeldner, Maurice
N1 - Keywords: Animals; Benzodiazepines; Binding Sites; Brain; Chalcones; Flavonoids; Fluorides; Ligands; Male; Phosphates; Polycyclic Hydrocarbons, Aromatic; Rats; Rats, Wistar; Receptors, GABA-A; Salts
PY - 2008
Y1 - 2008
N2 - 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.
AB - 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.
KW - Former Faculty of Pharmaceutical Sciences
U2 - 10.1016/j.bmcl.2008.07.107
DO - 10.1016/j.bmcl.2008.07.107
M3 - Journal article
C2 - 18707883
VL - 18
SP - 4864
EP - 4867
JO - Bioorganic & Medicinal Chemistry Letters
JF - Bioorganic & Medicinal Chemistry Letters
SN - 0960-894X
IS - 17
ER -
ID: 10161334