| Literature DB >> 19783443 |
Kenneth N Mewett1, Sebastian P Fernandez, Anmol K Pasricha, Alice Pong, Steven O Devenish, David E Hibbs, Mary Chebib, Graham A R Johnston, Jane R Hanrahan.
Abstract
We herein describe the synthesis and positive modulatory activities of a small library of flavan-3-ol derivatives on alpha(1)beta(2)gamma(2L) GABA(A) 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.Mesh:
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Year: 2009 PMID: 19783443 DOI: 10.1016/j.bmc.2009.08.062
Source DB: PubMed Journal: Bioorg Med Chem ISSN: 0968-0896 Impact factor: 3.641