Structure–activity studies on 1, 3-dioxane-2-carboxylic acid derivatives, a novel class of subtype-selective peroxisome proliferator-activated receptor α (PPARα) …

…, S Ohmachi, K Kuwabara, K Murakami, M Todo

Index: Asaki, Tetsuo; Aoki, Tomiyoshi; Hamamoto, Taisuke; Sugiyama, Yukiteru; Ohmachi, Shinji; Kuwabara, Kenji; Murakami, Kohji; Todo, Makoto Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 2 p. 981 - 994

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Citation Number: 28

Abstract

A series of 1, 3-dioxane carboxylic acid derivatives was synthesized and evaluated for human PPAR transactivation activity. Structure–activity relationships on the phenyloxazole moiety of the lead compound 3 revealed that the introduction of small hydrophobic substituents at the 4-position of the terminal phenyl ring increased the PPARα agonist activity, and that the oxazole heterocycle was essential to the maintenance of both ...