8 research outputs found

    Titanium-Promoted Acylation of Sulfonamides to <i>N</i>-Acylsulfonamide PPARα Antagonists

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    <div><p></p><p>The direct acylation of sulfonamides by esters represents an attractive strategy in organic chemistry, being an interesting alternative to classical approaches to <i>N</i>-acylsulfonamides. Here is described a simple and effective method to obtain <i>N</i>-acylsulfonamides of pharmaceutical interest, in a reaction promoted by titanium(IV) chloride. This strategy was successfully applied to the synthesis of a peroxisome proliferator–activated receptor α antagonist with a benzenesulfonimide moiety, ensuring an excellent yield of product. The reaction was further studied to explore the behavior of different α-bromoesters and esters and the effects of <i>para</i>-substitution in the benzenesulfonamide moiety.</p></div

    Effect of GW6471 on PI3K/GSK-3β/β-catenin signaling pathway in PTJ64i and PTJ86i cell lines.

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    <p>Histograms of normalized densitometric analyses and representative western blotting for PI3K, GSK3β, p-GSK3β and β-catenin in HNPGL cells treated with 24 μM GW6471 for 72 hours are shown. The relative densities of the immunoreactive bands were determined and normalized with respect to GAPDH (loading control) using a semiquantitative densitometric analysis (Kodak ID Image Analysis Software, Rochester, NY, USA). Values are expressed as relative units (RU). Each bar represents the mean ± SD of two up to five independent determinations (*<i>p</i><0.05).</p
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