Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175 was written by Piemontese, Luca;Fracchiolla, Giuseppe;Carrieri, Antonio;Parente, Mariagiovanna;Laghezza, Antonio;Carbonara, Giuseppe;Sblano, Sabina;Tauro, Marilena;Gilardi, Federica;Tortorella, Paolo;Lavecchia, Antonio;Crestani, Maurizio;Desvergne, Beatrice;Loiodice, Fulvio. And the article was included in European Journal of Medicinal Chemistry in 2015.Recommanded Product: 15399-05-0 This article mentions the following:
The effects resulting from the introduction of an oxime group in place of the distal aromatic ring of the di-Ph moiety of LT175, previously reported as a PPARα/γ dual agonist, have been investigated. This modification allowed the identification of new bioisosteric ligands with fairly good activity on PPARα and fine-tuned moderate activity on PPARγ. For the most interesting compound (S)-2-[4-(Propoxyimino-methyl)phenoxy]-3-phenylpropanoic acid ((S)-3), docking studies in PPARα and PPARγ provided a mol. explanation for its different behavior as full and partial agonist of the two receptor isotypes, resp. A further investigation of this compound was carried out performing gene expression studies on HepaRG cells. The results obtained allowed to hypothesize a possible mechanism through which this ligand could be useful in the treatment of metabolic disorders. The higher induction of the expression of some genes, compared to selective agonists, seems to confirm the importance of a dual PPARα/γ activity which probably involves a synergistic effect on both receptor subtypes. In the experiment, the researchers used many compounds, for example, Ethyl 2-hydroxy-3-phenylpropanoate (cas: 15399-05-0Recommanded Product: 15399-05-0).
Ethyl 2-hydroxy-3-phenylpropanoate (cas: 15399-05-0) belongs to esters. Esters perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market. Polyesters are important plastics, with monomers linked by ester moieties. Cyclic esters are called lactones, regardless of whether they are derived from an organic or inorganic acid. One example of an organic lactone is γ-valerolactone.Recommanded Product: 15399-05-0
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