524959-64-6Relevant academic research and scientific papers
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
Aleglitazar, a new, potent, and balanced dual PPARα/γ agonist for the treatment of type II diabetes
Benardeau, Agnes,Benz, Joerg,Binggeli, Alfred,Blum, Denise,Boehringer, Markus,Grether, Uwe,Hilpert, Hans,Kuhn, Bernd,Maerki, Hans Peter,Meyer, Markus,Puentener, Kurt,Raab, Susanne,Ruf, Armin,Schlatter, Daniel,Mohr, Peter
scheme or table, p. 2468 - 2473 (2010/03/24)
Design, synthesis, and SAR of novel α-alkoxy-β-arylpropionic acids as potent and balanced PPARαγ coagonists are described. One representative thereof, Aleglitazar ((S)-2Aa), was chosen for clinical development. Its X-ray structure in complex with both receptors as well as its high efficacy in animal models of T2D and dyslipidemia are also presented.
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
IMPROVED PROCESS FOR PREPARING OXAZOLE NITRILES
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Page/Page column 7, (2008/06/13)
An improved process for preparing oxazole nitriles of formula (I) in which Ar is aryl or heteroaryl and Rl is H or alkyl , which comprises reacting a corresponding oxazole chloride of formula (II) in which Ar and Rl are as defined above, in a solvent with
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.
