Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 17, Issue 20, Pages 7156-7173Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.08.062
Keywords
GABA(A); Flavan-3-ol; Positive modulator; Structure-activity
Funding
- National Health and Medical Research Council (NHMRC) of Australia
- Australian Postgraduate Award
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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. (C) 2009 Elsevier Ltd. All rights reserved.
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