Design and Synthesis of 3-(2-Ethyl-4-{2-[2-(4-fluorophenyl)-5-methyloxazol-4-yl]ethoxy}phenyl)propanoic Acid: A Novel Triple-acting PPARα, -γ, and -δ Agonist

The design and synthesis of triple-acting PPARα, -γ, and -δ agonist 3-(2-ethyl-4-{2-[2-(4-fluorophenyl)-5-methyloxazol-4-yl]ethoxy}phenyl)propanoic acid (1a) is described. The compound possesses a potent triple-acting PPARα, -γ, and -δ agonist profile with an EC50 of 0.029, 0.013, and 0.029 µM, resp...

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Bibliographic Details
Published in:Chemistry letters 2012-04, Vol.41 (4), p.406-408
Main Authors: Zhang, Qijun, Sun, Peng, Zheng, Guojun, Wang, Yaping, Wang, Xiangjing, Wei, Hegeng, Xiang, Wensheng
Format: Article
Language:English
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Summary:The design and synthesis of triple-acting PPARα, -γ, and -δ agonist 3-(2-ethyl-4-{2-[2-(4-fluorophenyl)-5-methyloxazol-4-yl]ethoxy}phenyl)propanoic acid (1a) is described. The compound possesses a potent triple-acting PPARα, -γ, and -δ agonist profile with an EC50 of 0.029, 0.013, and 0.029 µM, respectively. The synthetic route, involving the synthesis of oxazole rings as the key step, starts from commercially available 3-oxopentanoic acid methyl ester and 3-hydroxyacetophenone to afford the target compound 1 with an overall yield of 32%.
ISSN:0366-7022
1348-0715
DOI:10.1246/cl.2012.406