Synthesis and biological evaluation of flavan-3-ol derivatives as positive modulators of GABAA receptors |
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| Authors: | Kenneth N Mewett Sebastian P Fernandez Anmol K Pasricha Alice Pong Steven O Devenish David E Hibbs Mary Chebib Graham AR Johnston Jane R Hanrahan |
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| Institution: | 1. Adrien Albert Laboratory of Medicinal Chemistry, Department of Pharmacology, Faculty of Medicine, The University of Sydney, NSW 2006, Australia;2. Pharmaceutical Chemistry, Faculty of Pharmacy, The University of Sydney, NSW 2006, Australia |
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| 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. |
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