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ID: ALA1933028
Journal: Bioorg Med Chem Lett
Title: Discovery of cyclic amine-substituted benzoic acids as PPARα agonists.
Authors: Nomura M, Yumoto K, Shinozaki T, Isogai S, Takano Y, Murakami K.
Abstract: 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.
CiteXplore: 22133631