Discovery of a novel class of 1, 3-dioxane-2-carboxylic acid derivatives as subtype-selective peroxisome proliferator-activated receptor α (PPARα) agonists

…, T Asaki, T Hamamoto, Y Sugiyama, S Ohmachi…

文献索引：Aoki, Tomiyoshi; Asaki, Tetsuo; Hamamoto, Taisuke; Sugiyama, Yukiteru; Ohmachi, Shinji; Kuwabara, Kenji; Murakami, Kohji; Todo, Makoto Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 6 p. 2128 - 2132

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被引用次数: 9

摘要

A new series of 1, 3-dioxane-2-carboxylic acid derivatives was synthesized and evaluated for agonist activity at human peroxisome proliferator-activated receptor (PPAR) subtypes. Structure-activity relationship studies led to the identification of 2-methyl-c-5-[4-(5-methyl-2- phenyl-1, 3-oxazol-4-yl) butyl]-1, 3-dioxane-r-2-carboxylic acid 4b as a potent PPARα agonist with high subtype selectivity at human receptor subtypes. This compound ...