Identification of novel PPARalpha ligands by the structural modification of a PPARgamma ligand.
To develop novel PPARalpha ligands, we designed and synthesized several 3-{3-[2-(nonylpyridin-2-ylamino)ethoxy]phenyl}propanoic acid derivatives. Compound 10, the meta isomer of a PPARgamma agonist 1, has been identified as a PPARalpha ligand. The introduction of methyl and ethyl groups at the C-2 position of the propanoic acid of 10 further improved the PPARalpha-binding potency.
Usui
Shinya
S
Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan.
Fujieda
Hiroki
H
Suzuki
Takayoshi
T
Yoshida
Naoaki
N
Nakagawa
Hidehiko
H
Miyata
Naoki
N
D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D047493:PPAR alpha / Q000737:chemistry* / Q000378:metabolism*; D047495:PPAR gamma / Q000737:chemistry* / Q000378:metabolism*; D013329:Structure-Activity Relationship
D008024:Ligands; D047493:PPAR alpha; D047495:PPAR gamma