Phenylpropanoic acid derivatives bearing a benzothiazole ring as PPARdelta-selective agonists.
To find novel PPARdelta-selective agonists, we designed and synthesized phenylpropanoic acid derivatives bearing 6-substituted benzothiazoles. Optimization of this series led to the identification of a potent and selective PPARdelta agonist 17. Molecular modeling suggested that compound 17 occupies the Y-shaped pocket of PPARdelta appropriately.
Fujieda
Hiroki
H
Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan.
Usui
Shinya
S
Suzuki
Takayoshi
T
Nakagawa
Hidehiko
H
Ogura
Michitaka
M
Makishima
Makoto
M
Miyata
Naoki
N
D052160:Benzothiazoles / Q000737:chemistry*; D006801:Humans; D008958:Models, Molecular; D047494:PPAR delta / Q000819:agonists*; D010666:Phenylpropionates / Q000494:pharmacology*; D011743:Pyrimidines / Q000494:pharmacology
D052160:Benzothiazoles; D047494:PPAR delta; D010666:Phenylpropionates; D011743:Pyrimidines; C006253:pirinixic acid