524959-64-6Relevant articles and documents
Design and synthesis of Oxime ethers of β-oxo-γ-phenylbutanoic acids as PPAR a and -γ dual agonists
Han, Hee Oon,Koh, Jong Sung,Kim, Seung Hae,Park, Ok Ku,Kim, Kyoung-Hee,Jeon, Sang Kweon,Hur, Gwong-Cheung,Yim, Hyeon Joo,Kim, Geun Tae
, p. 1979 - 1982 (2012/08/14)
Oxime ethers of p-oxo-y-phenylbutanoic acids were prepared to develop more effective PPAR a and y dual agonists. Among them, compound 11k exhibited potent in vitro activities with EC50 of 2.5 nM and 3.3 nM in PPAR a and y, respectively. It showed better g
Design and synthesis of oxime ethers of α-acyl-β-phenylpropanoic acids as PPAR dual agonists
Oon Han, Hee,Hae Kim, Seung,Kim, Kyoung-Hee,Hur, Gwong-Cheung,Joo Yim, Hyeon,Chung, Hee-Kyung,Ho Woo, Sung,Dong Koo, Ki,Lee, Chang-Seok,Sung Koh, Jong,Tae Kim, Geun
, p. 937 - 941 (2007/10/03)
Oxime ethers of α-acyl-β-phenylpropanoic acids were prepared to apply as PPARα and γ dual agonists. Among them, compound 11l proved to exhibit potent in vitro activities with EC50 of 19 and 13 nM in PPARα and γ, respectively. It showed better g
Conversion of human-selective PPARα agonists to human/mouse dual agonists: A molecular modeling analysis
Wang, Minmin,Winneroski, Leonard L.,Ardecky, Robert J.,Babine, Robert E.,Brooks, Dawn A.,Etgen, Garret J.,Hutchison, Darrell R.,Kauffman, Raymond F.,Kunkel, Aaron,Mais, Dale E.,Montrose-Rafizadeh, Chahrzad,Ogilvie, Kathleen M.,Oldham, Brian A.,Peters, Mary K.,Rito, Christopher J.,Rungta, Deepa K.,Tripp, Allie E.,Wilson, Sarah B.,Xu, Yanping,Zink, Richard W.,McCarthy, James R.
, p. 6113 - 6116 (2007/10/03)
To understand the species selectivity in a series of α-methyl- α-phenoxy carboxylic acid PPARα/γ dual agonists (1-11), structure-based molecular modeling was carried out in the ligand binding pockets of both human and mouse PPARα. This study suggested that interaction of both 4-phenoxy and phenyloxazole substituents of these ligands with F272 and M279 in mouse PPARα leads to the species-specific divergence in ligand binding. Insights obtained in the molecular modeling studies of these key interactions resulted in the ability to convert a human-selective PPARα agonist to a human and mouse dual agonist within the same platform.