Design and Synthesis of 2-Methyl-2-{4-[2-(5-methyl-2-aryloxazol- 4-yl)ethoxy]phenoxy}propionic Acids:  A New Class of Dual PPARα/γ Agonists

Propionic acid derivative 8, which was designed and synthesized based on putative pharmacophores of known PPARγ- and PPARα-selective compounds, exhibits potent dual PPARα/γ agonist activity as demonstrated by in vitro binding and dose overlap in the newly introduced EOB mouse model for glucose lower...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2001-06, Vol.44 (13), p.2061-2064
Main Authors: Brooks, Dawn A, Etgen, Garret J, Rito, Christopher J, Shuker, Anthony J, Dominianni, Samuel J, Warshawsky, Alan M, Ardecky, Robert, Paterniti, James R, Tyhonas, John, Karanewsky, Donald S, Kauffman, Raymond F, Broderick, Carol L, Oldham, Brian A, Montrose-Rafizadeh, Chahzrad, Winneroski, Leonard L, Faul, Margaret M, McCarthy, James R
Format: Article
Language:English
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Summary:Propionic acid derivative 8, which was designed and synthesized based on putative pharmacophores of known PPARγ- and PPARα-selective compounds, exhibits potent dual PPARα/γ agonist activity as demonstrated by in vitro binding and dose overlap in the newly introduced EOB mouse model for glucose lowering and lipid/cholesterol homeostasis.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm0155188