4.5 Article

Design, total synthesis, and biological evaluation of neodysiherbaine A derivative as potential probes

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 22, 页码 5784-5787

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.08.082

关键词

AMPA receptors; excitatory amino acid; glutamate receptors; kainate receptors; dysiherbaine; neodysiherbaine A; total synthesis

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To enable studies to elucidate the detailed biological function of dysiherbaine and neodysiherbaine A, potent and subunit-selective agonists for ionotropic glutamate receptors, the derivative with a hydroxymethyl substituent at the C10 position has been developed. Preliminary biological evaluation of the analogue showed that a C10 hydroxymethyl substituent produced significant alterations in binding affinities for the ionotropic glutamate receptor subtypes. (c) 2006 Elsevier Ltd. All rights reserved.

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