876148-26-4Relevant articles and documents
Discovery of cyclic amine-substituted benzoic acids as PPARα agonists
Nomura, Masahiro,Yumoto, Kazuhiro,Shinozaki, Takehiro,Isogai, Shigeki,Takano, Yasuo,Murakami, Koji
, p. 334 - 338 (2012/02/15)
A series of novel cyclic amine-substituted benzoic acid derivatives were synthesized and evaluated for their PPARα agonist activity. Strucure-activity relationship studies led to the identification of (S)-3-[3-[2-(4-chlorophenyl)-4-methylthyazole-5-carboxamido]piperidin-1-yl] benzoic acid (S)-4f (KRP-105) as a potent and high subtype-selective human PPARα agonist. (S)-4f showed excellent PK profile and oral administration of (S)-4f to high-fat diet dogs effectively lowered triglycerides.