334015-34-8Relevant academic research and scientific papers
Design, synthesis, and evaluation of potent, structurally novel peroxisome proliferator-activated receptor (PPAR) δ-selective agonists
Kasuga, Jun-ichi,Nakagome, Izumi,Aoyama, Atsushi,Sako, Kumiko,Ishizawa, Michiyasu,Ogura, Michitaka,Makishima, Makoto,Hirono, Shuichi,Hashimoto, Yuichi,Miyachi, Hiroyuki
, p. 5177 - 5190 (2008/03/14)
A series of 3-(4-alkoxyphenyl)propanoic acid derivatives was prepared as candidate peroxisome proliferator-activated receptor (PPAR) δ-selective agonists, based on our previously discovered potent human PPARα/δ dual agonist TIPP-401 as a lead compound. Structure-activity relationship studies clearly indicated the importance of the chain length of the alkoxy group at the 4-position, and the n-butoxy compound exhibited the most potent PPARδ transactivation activity and highest PPARδ selectivity. The (S)-enantiomer of a representative compound exhibited extremely potent PPARδ transactivation activity, comparable with or somewhat superior to that of the known PPARδ-selective agonist, GW-501516. The representative compound regulated the expression of genes involved in lipid and glucose homeostasis, and should be useful not only as a chemical tool to study PPARδ function, but also as a candidate drug for the treatment of metabolic syndrome.
Design, synthesis, and evaluation of a novel series of α-substituted phenylpropanoic acid derivatives as human peroxisome proliferator-activated receptor (PPAR) α/δ dual agonists for the treatment of metabolic syndrome
Kasuga, Jun-ichi,Yamasaki, Daisuke,Araya, Yoko,Nakagawa, Aya,Makishima, Makoto,Doi, Takefumi,Hashimoto, Yuichi,Miyachi, Hiroyuki
, p. 8405 - 8414 (2008/02/05)
A series of α-alkyl-substituted phenylpropanoic acids was prepared as dual agonists of peroxisome proliferator-activated receptors alpha and delta (PPARα/δ). Structure-activity relationship studies indicated that the shape of the linking group and the sha
Design, synthesis, and evaluation of substituted phenylpropanoic acid derivatives as human peroxisome proliferator activated receptor activators. Discovery of potent and human peroxisome proliferator activated receptor α subtype-selective activators
Nomura, Masahiro,Tanase, Takahiro,Ide, Tomohiro,Tsunoda, Masaki,Suzuki, Masahiro,Uchiki, Hideharu,Murakami, Koji,Miyachi, Hiroyuki
, p. 3581 - 3599 (2007/10/03)
Substituted phenylpropanoic acid derivatives were prepared as part of a search for subtype-selective human peroxisome proliferator activated receptor α (PPARα) activators. Structure-activity relationship studies indicated that the nature and the stereoche
Substituted phenylpropionic acid derivatives
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, (2008/06/13)
The invention provides novel substituted phenylpropionic acid derivatives that bind to the receptor as ligands of human peroxisome proliferator-activated receptor a (PPARα) to activate and exhibit potent lipid-decreasing action, and processes for preparin
