- Discovery of a novel class of PPARdelta partial agonists.
Discovery of a novel class of PPARdelta partial agonists.
Bioorganic & medicinal chemistry letters (2008-08-30)
Barry G Shearer, Hari S Patel, Andrew N Billin, James M Way, Deborah A Winegar, Millard H Lambert, Robert X Xu, Lisa M Leesnitzer, Raymond V Merrihew, Stephane Huet, Timothy M Willson
PMID18722772
ABSTRACT
Anthranilic acid GW9371 was identified as a novel class of PPARdelta partial agonist through high-throughput screening. The design and synthesis of SAR analogues is described. GSK1115 and GSK7227 show potent partial agonism of the PPARdelta target genes CPT1a and PDK4 in skeletal muscle cells.
MATERIALS