Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1363546 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
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 pEC50 = 9). Details of the SAR and optimization of this series are presented herein.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Brian W. Budzik, Karen A. Evans, David D. Wisnoski, Jian Jin, Ralph A. Rivero, George R. Szewczyk, Channa Jayawickreme, David L. Moncol, Hongshi Yu,