Author/Authors :
Kenneth N. Mewett، نويسنده , , Sebastian P. Fernandez، نويسنده , , Anmol K. Pasricha، نويسنده , , Alice Pong، نويسنده , , Steven O. Devenish، نويسنده , , David E. Hibbs، نويسنده , , Mary Chebib، نويسنده , , Graham A.R. Johnston، نويسنده , , Jane R. Hanrahan، نويسنده ,
Abstract :
We herein describe the synthesis and positive modulatory activities of a small library of flavan-3-ol derivatives on α1β2γ2L GABAA receptors. Structure–activity relationships of various substituents on the A, B and C rings were evaluated in a functional electrophysiological assay. A trans configuration and a 3-acetoxy moiety are essential for activity. Substitution of the B ring appears to be well tolerated, with substituents on the A ring playing a major role in determining activity.
Keywords :
Flavan-3-ol , structure–activity , Positive modulator , GABAA
