223125-74-4Relevant articles and documents
Synthesis and biological activity of novel α-substituted β-phenylpropionic acids having pyridin-2-ylphenyl moiety as antihyperglycemic agents
Takamura, Makoto,Sakurai, Mitsuya,Yamada, Eriko,Fujita, Sachie,Yachi, Makoto,Takagi, Toshiyuki,Isobe, Aya,Hagisawa, Yuka,Fujiwara, Toshihiko,Yanagisawa, Hiroaki
, p. 2419 - 2439 (2007/10/03)
We previously reported the identification of novel oximes having 5-benzyl-2,4-thiazolidinedione with antihyperglycemic activity. We now report the synthesis and biological activity of a novel series of oximes and amides having α-substituted-β-phenylpropionic acids. In this series, we obtained potent PPARα/γ dual agonist (S)-9d, with which activation of PPARα and PPARγ was considerably more potent than that of the reference compounds GW9578 22 and rosiglitazone 3, respectively. This means (S)-9d is of the strongest class of PPARα/γ dual agonists. In the course of this study, we also obtained 8h, which indicated potent plasma glucose lowering effect in spite of weak PPARα/γ agonistic activity.