Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 4, Pages 1363-1367Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.01.003
Keywords
SAR; TGR5; TGR5 agonists; GPCR; Solution-phase synthesis
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A series of 3-aryl-4-isoxazolecarboxamides identified from a high-throughput screening campaign as novel, potent agonists of the human TGR5 G-protein-coupled receptor is described. Many analogues were readily accessible via solution-phase synthesis which resulted in the rapid identification of key structure activity relationships (SAR), and the discovery of potent exemplars (up to pEC(50) = 9). Details of the SAR and optimization of this series are presented herein. (C) 2010 Elsevier Ltd. All rights reserved.
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