Bioorganic & Medicinal Chemistry Letters 2008-09-15

Discovery of a novel class of PPARdelta partial agonists.

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

Index: Bioorg. Med. Chem. Lett. 18 , 5018, (2008)

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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.