378232-23-6Relevant articles and documents
Structure-based design, synthesis, and nonalcoholic steatohepatitis (NASH)-preventive effect of phenylpropanoic acid peroxisome proliferator- activated receptor (PPAR) α-selective agonists
Ban, Shintaro,Kasuga, Jun-Ichi,Nakagome, Izumi,Nobusada, Hiromi,Takayama, Fusako,Hirono, Shuichi,Kawasaki, Hiromu,Hashimoto, Yuichi,Miyachi, Hiroyuki
, p. 3183 - 3191 (2011/06/24)
A series of α-ethylphenylpropanoic acid derivatives was prepared as candidate peroxisome proliferator-activated receptor (PPAR) α-selective agonists, based on our PPARα/δ dual agonist 3 as a lead compound. Structure-activity relationship studies clearly indicated that the steric bulkiness and position of the distal hydrophobic tail part are critical for PPARα agonistic activity and PPARα selectivity, as had been predicted from a molecular-modeling study. A representative compound blocked the progression of nonalcoholic steatohepatitis (NASH) in an animal model.
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.
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