Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 15, Issue 5, Pages 1311-1313Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.01.025
Keywords
estrogen-related receptor; nuclear hormone receptor; agonist
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In order to develop agonist ligands that are specific for the estrogen-related receptors ERR beta/gamma, a hydrazone with a 4-hydroxy group at one phenyl ring and a 4-diethylamino moiety at the other phenyl ring was synthesized. We demonstrate that compound 3 (DY131; N'-{(1E)-[4-(diethylamino)phenyl]methylene}-4-hydroxybenzohydrazide) effectively and selectively activates ERR beta/gamma. DY131 had no effect on the structurally related receptors ERR alpha or the estrogen receptors alpha and beta (ER alpha/beta). This work defines a convenient synthesis for a novel and selective pharmacologic tool that can be used to elucidate the biological activities of ERR beta/gamma. (c) 2005 Elsevier Ltd. All rights reserved.
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