1, 3, 5-Trisubstituted aryls as highly selective PPARδ agonists

R Epple, M Azimioara, R Russo, B Bursulaya…

Index: Epple, Robert; Azimioara, Mihai; Russo, Ross; Bursulaya, Badry; Tian, Shin-Shay; Gerken, Andrea; Iskandar, Maya Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 11 p. 2969 - 2973

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Citation Number: 37

Abstract

A series of highly potent and selective PPARδ agonists is described using the known non- selective ligand GW2433 as a structural template. Compound 1 is bioavailable, potent (10nM), and shows no cross-activity with other PPAR subtypes up to 10μM, making it a useful tool in studying the biological effects of selective PPARδ activation.