Novel biphenylcarboxylic acid peroxisome proliferator-activated receptor (PPAR) δ selective antagonists

J Kasuga, S Ishida, D Yamasaki, M Makishima…

文献索引：Kasuga, Jun-ichi; Ishida, Seiichi; Yamasaki, Daisuke; Makishima, Makoto; Doi, Takefumi; Hashimoto, Yuichi; Miyachi, Hiroyuki Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 23 p. 6595 - 6599

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被引用次数: 20

摘要

We designed and synthesized novel PPARδ antagonists based on the crystal structure of the PPARδ full agonist TIPP-204 bound to the PPARδ ligand-binding domain, in combination with our nuclear receptor helix 12 folding modification hypothesis. Representative compound 3a exhibits PPARδ-preferential antagonistic activity.