Synthesis and structure–activity relationships of a series of 3-aryl-4-isoxazolecarboxamides as a new class of TGR5 agonists
作者:Brian W. Budzik、Karen A. Evans、David D. Wisnoski、Jian Jin、Ralph A. Rivero、George R. Szewczyk、Channa Jayawickreme、David L. Moncol、Hongshi Yu
DOI:10.1016/j.bmcl.2010.01.003
日期:2010.2
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.
1112. Derivatives of 6-aminopenicillanic acid. Part VI. Penicillins from 3- and 5-phenylisoxazole-4-carboxylic acids and their alkyl and halogen derivatives
作者:F. P. Doyle、J. C. Hanson、A. A. W. Long、J. H. C. Nayler、E. R. Stove