Design and synthesis of 2-methyl-2-{4-[2-(5-methyl-2-aryloxazol-4-yl)ethoxy]phenoxy}propionic acids: A new class of dual PPAR alpha/gamma agonists

Authors
Brooks, DA Etgen, GJ Rito, CJ Shuker, AJ Dominianni, SJ Warshawsky, AM Ardecky, R Paterniti, JR Tyhonas, J Karanewsky, DS Kauffman, RF Broderick, CL Oldham, BA Montrose-Rafizadeh, C Winneroski, LL Faul, MM McCarthy, JR
Citation
Da. Brooks et al., Design and synthesis of 2-methyl-2-{4-[2-(5-methyl-2-aryloxazol-4-yl)ethoxy]phenoxy}propionic acids: A new class of dual PPAR alpha/gamma agonists, J MED CHEM, 44(13), 2001, pp. 2061-2064
Citations number
23
Categorie Soggetti
Chemistry & Analysis
Journal title
JOURNAL OF MEDICINAL CHEMISTRY
ISSN journal
00222623 → ACNP
Volume
44
Issue
13
Year of publication
2001
Pages
2061 - 2064
Database
ISI
SICI code
0022-2623(20010621)44:13<2061:DASO2>2.0.ZU;2-U
Abstract
Propionic acid derivative 8, which was designed and synthesized based on pu tative pharmacophores of known PPAR gamma- and PPAR alpha -selective compou nds, exhibits potent dual PPAR alpha/gamma agonist activity as demonstrated by in vitro binding and dose overlap in the newly introduced EOB mouse mod el for glucose lowering and lipid/cholesterol homeostasis.