Design and synthesis of highly potent and selective human peroxisome proliferator-activated receptor alpha agonists.
A combination of benzoxazole, phenoxyalkyl side chain, and phenoxybutyric acids was identified as a highly potent and selective human peroxisome proliferator-activated receptor alpha (PPARalpha) agonist. The synthesis, structure-activity relationship (SAR) studies, and in vivo activities of the representative compounds are described.
Yamazaki
Yukiyoshi
Y
Tokyo New Drug Research Laboratories 1, Pharmaceutical Division, Kowa Co., LTD, 2-17-43, Noguchicho, Higashimurayam, Tokyo 189-0022, Japan. y-yamazk@kowa.co.jp
Abe
Kazutoyo
K
Toma
Tsutomu
T
Nishikawa
Masahiro
M
Ozawa
Hidefumi
H
Okuda
Ayumu
A
Araki
Takaaki
T
Oda
Soichi
S
Inoue
Keisuke
K
Shibuya
Kimiyuki
K
Staels
Bart
B
Fruchart
Jean-Charles
JC
D000485:Allergens; D000818:Animals; D052179:Antigens, Plant; D015195:Drug Design; D006571:Heterocyclic Compounds / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D000960:Hypolipidemic Agents / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D008822:Mice, Transgenic; D015394:Molecular Structure; D047493:PPAR alpha / Q000819:agonists*; D010940:Plant Proteins; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
D000485:Allergens; D052179:Antigens, Plant; D006571:Heterocyclic Compounds; D000960:Hypolipidemic Agents; C095551:MALD1 protein, Malus domestica; D047493:PPAR alpha; D010940:Plant Proteins