1609109-71-8Relevant articles and documents
Identification of the first potent, selective and bioavailable PPARα antagonist
Bravo, Yalda,Baccei, Christopher S.,Broadhead, Alex,Bundey, Richard,Chen, Austin,Clark, Ryan,Correa, Lucia,Jacintho, Jason D.,Lorrain, Daniel S.,Messmer, Davorka,Stebbins, Karin,Prasit, Peppi,Stock, Nicholas
, p. 2267 - 2272 (2014/05/20)
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.
