Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369040 | Bioorganic & Medicinal Chemistry Letters | 2014 | 6 Pages |
Abstract
The discovery and SAR of a novel series of potent and selective PPARα antagonists are herein described. Exploration of replacements for the labile acyl sulfonamide linker led to a biaryl sulfonamide series of which compound 33 proved to be suitable for further profiling in vivo. Compound 33 demonstrated excellent potency, selectivity against other nuclear hormone receptors, and good pharmacokinetics in mouse.
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Related Topics
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Authors
Yalda Bravo, Christopher S. Baccei, Alex Broadhead, Richard Bundey, Austin Chen, Ryan Clark, Lucia Correa, Jason D. Jacintho, Daniel S. Lorrain, Davorka Messmer, Karin Stebbins, Peppi Prasit, Nicholas Stock,